| Adenosine A1 receptor |
Ki |
= |
600.0 |
nM |
Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. |
CHEMBL1124694 |
| Adenosine A2 receptor |
Ki |
= |
116.0 |
nM |
Inhibition of binding of [3H]NECA to adenosine A2 receptor of rat striatal membranes. |
CHEMBL1124694 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
0.19 |
|
Selectivity ratio for A1 receptor to that of A2 receptor in vitro in rat tissues |
CHEMBL1124694 |
| Adenosine A1 receptor |
Ki |
= |
600.0 |
nM |
Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. |
CHEMBL1124142 |
| Adenosine A2 receptor |
Ki |
= |
116.0 |
nM |
Binding affinity at adenosine A2 receptor from rat striatal membranes by [3H]NECA displacement. |
CHEMBL1124142 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
0.19 |
|
Ratio of binding affinity against A2 and A1 receptors |
CHEMBL1124142 |
| Adenosine A1 receptor |
Ki |
= |
590.0 |
nM |
Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine |
CHEMBL1124304 |
| Adenosine A2 receptor |
Ki |
= |
120.0 |
nM |
Binding affinity towards adenosine A2 receptor on rat striatal membrane using [3H]NECA as radioligand |
CHEMBL1124304 |
| Adenosine A1 receptor |
EC25 |
= |
7000.0 |
nM |
Reduction of heart rate (A1 response) in isolated rat heart preparation |
CHEMBL1124304 |
| Adenosine A2 receptor |
EC25 |
= |
3.0 |
nM |
Enhancement of coronary flow (A2 response) in isolated rat heart preparation |
CHEMBL1124304 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
0.21 |
|
Ratio of Ki at adenosine A2 and A1 receptors |
CHEMBL1124304 |
| Adenosine A1 receptor |
Ki |
= |
689.0 |
nM |
Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine |
CHEMBL1124836 |
| Adenosine A2 receptor |
Ki |
= |
71.0 |
nM |
Binding to Adenosine A2 receptor was measured in ADA-pretreated rat striatal membranes using [3H]-CGS- 21680 |
CHEMBL1124836 |
| Rattus norvegicus |
EC25 |
= |
110.0 |
nM |
Effective concentration required for 25% increase in coronary flow(CF) in perfused working heart model was determined |
CHEMBL1124836 |
| Rattus norvegicus |
EC25 |
> |
3000.0 |
nM |
Effective concentration required for 25% increase in heart rate in perfused working heart model was determined |
CHEMBL1124836 |
| Unchecked |
Ratio |
= |
9.7 |
|
Ratio of A1-receptor binding to that of A2-receptor binding |
CHEMBL1124836 |
| Adenosine A1 receptor |
Ki |
= |
560.0 |
nM |
Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand |
CHEMBL1125572 |
| Adenosine A2 receptor |
Ratio |
= |
119.0 |
nM |
Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand |
CHEMBL1125572 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
0.21 |
|
Ratio of A2 to A1. |
CHEMBL1125572 |
| Adenosine A1 receptor |
Ki |
= |
780.0 |
nM |
Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand |
CHEMBL1126140 |
| Adenosine A2 receptor |
Ki |
= |
107.0 |
nM |
Binding affinity against adenosine A2 receptor in rat striatal membranes using [3H]NECA as radioligand |
CHEMBL1126140 |
| Rattus norvegicus |
ED30 |
= |
5.82 |
ug kg-1 |
Dose producing 30% decrease of blood pressure in anesthetized rats (SHR) |
CHEMBL1126140 |
| Rattus norvegicus |
ED10 |
> |
100.0 |
ug kg-1 |
Dose producing 10% decrease of heart rate in anesthetized rats (SHR) |
CHEMBL1126140 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
7.3 |
|
Selectivity against adenosine A1 to A2 receptors |
CHEMBL1126140 |
| Adenosine A1 receptor |
IC50 |
= |
1380.0 |
nM |
Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor |
CHEMBL1125861 |
| Adenosine A2 receptor |
IC50 |
= |
145.0 |
nM |
Concentration required for 50% inhibition of [3H]NECA binding on rat brain adenosine A2 receptor |
CHEMBL1125861 |
| Rattus norvegicus |
ED25 |
= |
0.029 |
mg kg-1 |
25% reduction in blood pressure in the rat. |
CHEMBL1125861 |
| Rattus norvegicus |
Delta HR |
= |
10.5 |
% |
Change in heart rate was expressed in percent at at a dose 0.29 mg/kg iv in anesthetized rat |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
165.0 |
mmHg |
Mean arterial pressure were recorded as baseline prior to the drug administration in hypertensive rats at 0.3 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
-33.0 |
mmHg |
Mean arterial pressure were recorded as change after 6 hr of following oral dosing hypertensive rats at 0.3 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
409.0 |
mmHg |
Heart rate was recorded as baseline prior to the drug administration in hypertensive rats at 0.3 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
25.0 |
mmHg |
Heart rate was recorded as change after 6 h of following oral dosing hypertensive rats at 0.3 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
180.0 |
mmHg |
Mean arterial pressure were recorded as baseline prior to the drug administration in hypertensive rats at 1.0 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
-45.0 |
mmHg |
Mean arterial pressure were recorded as change after 6 hr of following oral dosing hypertensive rats at 1.0 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
391.0 |
mmHg |
Heart rate was recorded as baseline prior to the drug administration in hypertensive rats at 1.0 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
66.0 |
mmHg |
Heart rate was recorded as change after 6 hr of following oral dosing hypertensive rats at 1.0 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
170.0 |
mmHg |
Mean arterial pressure were recorded as baseline prior to the drug administration in hypertensive rats at 3.0 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
-43.0 |
mmHg |
Mean arterial pressure were recorded as change after 6 hr of following oral dosing hypertensive rats at 3.0 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
391.0 |
mmHg |
Heart rate was recorded as baseline prior to the drug administration in hypertensive rats at 3.0 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
42.0 |
mmHg |
Heart rate was recorded as change after 6 hr of following oral dosing hypertensive rats at 3.0 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
163.0 |
mmHg |
Heart rate was recorded as baseline prior to the drug administration in hypertensive rats at 10 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
-50.0 |
mmHg |
Heart rate was recorded as change after 6 h of following oral dosing hypertensive rats at 10 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
409.0 |
mmHg |
Heart rate was recorded as baseline prior to the drug administration in hypertensive rats at 10 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
38.0 |
mmHg |
Heart rate was recorded as change after 6 h of following oral dosing hypertensive rats at 10 mg/kg dose |
CHEMBL1125861 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
9.5 |
|
Ratio of IC50 values for A1 receptor binding to that of A2 receptor |
CHEMBL1125861 |
| Adenosine A1 receptor |
EC50 |
= |
12589.25 |
nM |
Prolongation of the stimulus-QRS interval by 50% of the maximum response at the adenosine A1 receptor in langendorff guinea pig heart preparation |
CHEMBL1125661 |
| Adenosine A2 receptor |
EC50 |
= |
18.2 |
nM |
Coronary arteries vasodilation at the adenosine A2 receptor in langendorff guinea pig heart preparation |
CHEMBL1125661 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
770.0 |
|
Ratio of EC50 stim-QRS (conduction block) and EC50 for vasodilation of coronary arteries |
CHEMBL1125661 |
| Adenosine A1 receptor |
Ki |
= |
529.0 |
nM |
Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. |
CHEMBL1125505 |
| Adenosine A2 receptor |
Ki |
= |
83.0 |
nM |
Binding affinity against adenosine A2 receptor from rat striatum using [3H]NECA as radioligand. |
CHEMBL1125505 |
| Rattus norvegicus |
ED30 |
= |
6.1 |
ug kg-1 |
Dose producing 30% decrease in blood pressure of anesthetized spontaneously hypertensive rats (SHR's) |
CHEMBL1125505 |
| Rattus norvegicus |
ED10 |
> |
100.0 |
ug kg-1 |
Dose producing 10% decrease in heart rate of anesthetized spontaneously hypertensive rats (SHR's) |
CHEMBL1125505 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
6.0 |
|
Selectivity determined as Ratio of Ki(nM) of A1 adenosine receptor to the Ki(nM) of A2 adenosine receptor |
CHEMBL1125505 |
| Unchecked |
Inhibition |
|
|
% |
Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay |
CHEMBL1255231 |
| Plasmodium falciparum |
IC50 |
= |
10000.0 |
nM |
Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay |
CHEMBL1255382 |
| Plasmodium falciparum |
IC50 |
= |
10000.0 |
nM |
Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay |
CHEMBL1255382 |
| Plasmodium falciparum |
IC50 |
= |
10000.0 |
nM |
Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay |
CHEMBL1255382 |
| Plasmodium falciparum |
IC50 |
= |
6309.57 |
nM |
Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay |
CHEMBL1255382 |
| Unchecked |
EC50 |
= |
224.0 |
nM |
PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhibitors of Platelet Dense Granule Release. (Class of assay: confirmatory) [Related pubchem assays: 1663 (Primary HTS), 1678 (Summary of Project)] |
CHEMBL1201862 |
| Luciferin 4-monooxygenase |
EC50 |
> |
112219.0 |
nM |
PUBCHEM_BIOASSAY: Luminescence Biochemical Dose Response HTS to Identify Inhibitors of Luciferase. (Class of assay: confirmatory) [Related pubchem assays: 1663 (Primary HTS), 1678 (Summary of Project)] |
CHEMBL1201862 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
651.0 |
nM |
PUBCHEM_BIOASSAY: Validation screen for small molecules that induce genotoxicity in human embryonic kidney (HEK293T) cells expressing luciferase-tagged ELG1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493143, AID504466] |
CHEMBL1201862 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Potency |
|
21192.3 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Histone Lysine Methyltransferase G9a. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504404] |
CHEMBL1201862 |
| 6-phospho-1-fructokinase |
Potency |
|
37933.0 |
nM |
PUBCHEM_BIOASSAY: qHTS Validation Assay to Find Inhibitors of T. brucei phosphofructokinase. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488768, AID492961] |
CHEMBL1201862 |
| Unchecked |
Potency |
|
46.1 |
nM |
PUBCHEM_BIOASSAY: qHTS Validation Assay to Find Inhibitors of Chronic Active B-Cell Receptor Signaling. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493014] |
CHEMBL1201862 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
5802.4 |
nM |
PUBCHEM_BIOASSAY: Validation screen for small molecules that inhibit ELG1-dependent DNA repair in human embryonic kidney (HEK293T) cells expressing luciferase-tagged ELG1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493125, AID504467] |
CHEMBL1201862 |
| Vitamin D receptor |
Potency |
|
44668.4 |
nM |
PUBCHEM_BIOASSAY: Inhibitors of the vitamin D receptor (VDR): qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504855] |
CHEMBL1201862 |
| Thioredoxin reductase 1, cytoplasmic |
Potency |
|
8912.5 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1): qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488771] |
CHEMBL1201862 |
| DNA polymerase iota |
Potency |
|
79432.8 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of Polymerase Iota. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588623] |
CHEMBL1201862 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
AC50 |
= |
6711.0 |
nM |
PUBCHEM_BIOASSAY: MLPCN Dyrk1A Kinase Measured in Biochemical System Using Plate Reader - 2124-01_Inhibitor_Dose_CherryPick_Activity. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504442] |
CHEMBL1201862 |
| Regulator of G-protein signaling 4 |
Potency |
|
5.3 |
nM |
PUBCHEM_BIOASSAY: Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504856] |
CHEMBL1201862 |
| Unchecked |
Potency |
|
1995.3 |
nM |
PubChem BioAssay. qHTS Assay for Inhibitors of Hepatitis C Virus (HCV). (Class of assay: confirmatory) |
CHEMBL1201862 |
| Geminin |
Potency |
|
35481.3 |
nM |
PubChem BioAssay. A quantitative high throughput screen for small molecules that induce DNA re-replication in SW480 colon adenocarcinoma cells. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Glucagon-like peptide 1 receptor |
Potency |
|
8912.5 |
nM |
PubChem BioAssay. qHTS of GLP-1 Receptor Inverse Agonists (Inhibition Mode). (Class of assay: confirmatory) |
CHEMBL1201862 |
| Transcriptional regulator ERG |
Potency |
|
3162.3 |
nM |
PubChem BioAssay. qHTS for Small Molecule Inhibitors of the ERG Ets/DNA interaction. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Ubiquitin carboxyl-terminal hydrolase 1 |
Potency |
|
501.2 |
nM |
PubChem BioAssay. Inhibitors of USP1/UAF1: Primary Screen. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A2a receptor |
Ki |
= |
100.0 |
nM |
Binding affinity to rat recombinant adenosine receptor A2a |
CHEMBL3259781 |
| Adenosine A2b receptor |
EC50 |
|
|
|
Agonist activity at human recombinant adenosine receptor A2b by cAMP assay |
CHEMBL3259781 |
| Adenosine A1 receptor |
Ki |
= |
400.0 |
nM |
Binding affinity to rat recombinant adenosine A1 receptor |
CHEMBL3259781 |
| Adenosine A3 receptor |
Ki |
|
|
|
Binding affinity to human recombinant adenosine A3 receptor |
CHEMBL3259781 |
| SARS-CoV-2 |
Inhibition |
= |
9.92 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging |
CHEMBL4303101 |
| Replicase polyprotein 1ab |
Inhibition |
= |
11.6 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
0.24 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| SARS-CoV-2 |
Inhibition |
= |
0.24 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| HEK-293T |
Cell Viability |
= |
0.49 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
-0.14 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.4 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
1.34 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.77 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.2 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.52 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.76 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.95 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
1.11 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
1.57 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
2.54 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.7 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.63 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.84 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.84 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.83 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.96 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.76 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.95 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
1.09 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.91 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
1.18 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
1.12 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.85 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.9 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.93 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.93 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.93 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
1.14 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Tyrosine-protein kinase ABL |
Delta TM |
= |
1.28 |
C |
Thermal Shift Assay. Domain: start/stop: S229-K512 |
CHEMBL4632348 |
| Serine/threonine-protein kinase Aurora-A |
Delta TM |
= |
0.48 |
C |
Thermal Shift Assay. Domain: start/stop: E122-S403 |
CHEMBL4632348 |
| Bromodomain-containing protein 4 |
Delta TM |
= |
-2.05 |
C |
Thermal Shift Assay. Domain: start/stop: N44-E168 |
CHEMBL4632348 |
| Peregrin |
Delta TM |
= |
-1.32 |
C |
Thermal Shift Assay. Domain: start/stop: M626-G740 |
CHEMBL4632348 |
| Cyclin-dependent kinase 2 |
Delta TM |
= |
0.19 |
C |
Thermal Shift Assay. Domain: start/stop: M1-L298 |
CHEMBL4632348 |
| Casein kinase I delta |
Delta TM |
= |
1.54 |
C |
Thermal Shift Assay. Domain: start/stop: M1-K294 |
CHEMBL4632348 |
| Fibroblast growth factor receptor 3 |
Delta TM |
= |
1.13 |
C |
Thermal Shift Assay. Domain: start/stop: P449-E759 |
CHEMBL4632348 |
| Glycogen synthase kinase-3 beta |
Delta TM |
= |
-0.23 |
C |
Thermal Shift Assay. Domain: start/stop: M26-R383 |
CHEMBL4632348 |
| MAP kinase ERK2 |
Delta TM |
= |
0.19 |
C |
Thermal Shift Assay. Domain: start/stop: M1-S360 |
CHEMBL4632348 |
| Transcription intermediary factor 1-alpha |
Delta TM |
= |
-0.31 |
C |
Thermal Shift Assay. Domain: start/stop: G861-E979 |
CHEMBL4632348 |
| Adenosine A2a receptor |
K |
= |
2.93 |
10^6/M/s |
Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as affinity on-rate by surface plasmon resonance assay |
CHEMBL5126601 |
| Adenosine A2a receptor |
K |
= |
0.027000000000000003 |
/s |
Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as affinity off-rate by surface plasmon resonance assay |
CHEMBL5126601 |
| Adenosine A2a receptor |
Kd |
= |
9.1 |
nM |
Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay |
CHEMBL5126601 |
| Adenosine A2a receptor |
Ki |
= |
76.0 |
nM |
Binding affinity to human wild type adenosine A2A receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assay |
CHEMBL5126601 |
| Type-1 angiotensin II receptor |
%Max (Mean) |
= |
-0.99 |
% |
GPCR beta-arrestin recruitment assay with target: AGTR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Type-1 angiotensin II receptor |
%Inhib (Mean) |
= |
-23.44 |
% |
GPCR beta-arrestin recruitment assay with target: AGTR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Adhesion G-protein coupled receptor F1 |
%Max (Mean) |
= |
12.97 |
% |
GPCR beta-arrestin recruitment assay with target: ADGRF1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Adhesion G-protein coupled receptor F1 |
%Inhib (Mean) |
= |
21.17 |
% |
GPCR beta-arrestin recruitment assay with target: ADGRF1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Sphingosine 1-phosphate receptor Edg-1 |
%Max (Mean) |
= |
-2.12 |
% |
GPCR beta-arrestin recruitment assay with target: S1PR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Sphingosine 1-phosphate receptor Edg-1 |
%Inhib (Mean) |
= |
-40.04 |
% |
GPCR beta-arrestin recruitment assay with target: S1PR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| C5a anaphylatoxin chemotactic receptor |
%Max (Mean) |
= |
-2.2880000000000003 |
% |
GPCR beta-arrestin recruitment assay with target: C5AR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| C5a anaphylatoxin chemotactic receptor |
%Inhib (Mean) |
= |
-9.74 |
% |
GPCR beta-arrestin recruitment assay with target: C5AR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| G-protein coupled receptor 120 |
%Max (Mean) |
= |
11.17 |
% |
GPCR beta-arrestin recruitment assay with target: FFAR4 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| G-protein coupled receptor 120 |
%Inhib (Mean) |
= |
-97.39 |
% |
GPCR beta-arrestin recruitment assay with target: FFAR4 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| G-protein coupled receptor 35 |
%Max (Mean) |
= |
-0.07732 |
% |
GPCR beta-arrestin recruitment assay with target: GPR35 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| G-protein coupled receptor 35 |
%Inhib (Mean) |
= |
-13.65 |
% |
GPCR beta-arrestin recruitment assay with target: GPR35 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Alpha-2a adrenergic receptor |
%Max (Mean) |
= |
-0.34 |
% |
GPCR beta-arrestin recruitment assay with target: ADRA2A Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Alpha-2a adrenergic receptor |
%Inhib (Mean) |
= |
-20.56 |
% |
GPCR beta-arrestin recruitment assay with target: ADRA2A Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Beta-2 adrenergic receptor |
%Max (Mean) |
= |
-2.81 |
% |
GPCR beta-arrestin recruitment assay with target: ADRB2 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Beta-2 adrenergic receptor |
%Inhib (Mean) |
= |
-26.09 |
% |
GPCR beta-arrestin recruitment assay with target: ADRB2 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Glucose-dependent insulinotropic receptor |
%Max (Mean) |
= |
-0.633 |
% |
GPCR beta-arrestin recruitment assay with target: GPR119 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Glucose-dependent insulinotropic receptor |
%Inhib (Mean) |
= |
-7.17 |
% |
GPCR beta-arrestin recruitment assay with target: GPR119 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Apelin receptor |
%Max (Mean) |
= |
-4.383 |
% |
GPCR beta-arrestin recruitment assay with target: APLNR Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Apelin receptor |
%Inhib (Mean) |
= |
7.17 |
% |
GPCR beta-arrestin recruitment assay with target: APLNR Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Lipoxin A4 receptor |
%Max (Mean) |
= |
-2.546 |
% |
GPCR beta-arrestin recruitment assay with target: FPR2 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Lipoxin A4 receptor |
%Inhib (Mean) |
= |
-24.96 |
% |
GPCR beta-arrestin recruitment assay with target: FPR2 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| C-X3-C chemokine receptor 1 |
%Max (Mean) |
= |
-3.05 |
% |
GPCR beta-arrestin recruitment assay with target: CX3CR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| C-X3-C chemokine receptor 1 |
%Inhib (Mean) |
= |
-46.72 |
% |
GPCR beta-arrestin recruitment assay with target: CX3CR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Glucagon-like peptide 1 receptor |
%Max (Mean) |
= |
-2.516 |
% |
GPCR beta-arrestin recruitment assay with target: GLP1R Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Glucagon-like peptide 1 receptor |
%Inhib (Mean) |
= |
-34.84 |
% |
GPCR beta-arrestin recruitment assay with target: GLP1R Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
