| Adenosine A1 receptor |
Ki |
= |
279.0 |
nM |
Binding affinity at rat Adenosine A1 receptor in the absence of GTP |
CHEMBL1135932 |
| Adenosine A1 receptor |
Ki |
= |
259.0 |
nM |
Binding affinity at rat Adenosine A1 receptor in the presence of GTP |
CHEMBL1135932 |
| Adenosine A1 receptor |
Ki |
= |
0.94 |
nM |
GTP-induced shift at rat Adenosine A1 receptor (A1AR) |
CHEMBL1135932 |
| Adenosine A1 receptor |
Ki |
= |
1185.0 |
nM |
Binding affinity at human Adenosine A1 receptor expressed in CHO cells |
CHEMBL1135932 |
| Adenosine A1 receptor |
Production |
= |
139.0 |
% |
Forskolin-induced cAMP production at human Adenosine A1 receptor receptor |
CHEMBL1135932 |
| Adenosine A1 receptor |
Ki |
= |
540.0 |
nM |
Binding affinity against adenosine A1 receptor in rat cortex by using [3H]- PIA as a radioligand |
CHEMBL1125213 |
| Adenosine A2 receptor |
Ki |
= |
11000.0 |
nM |
Binding affinity against adenosine A2 receptor in rat striatum by using [3H]NECA as a radioligand |
CHEMBL1125213 |
| Adenosine A2 receptor |
Ki |
= |
25000.0 |
nM |
Tested for inhibition of rat PC12 adenylate cyclase stimulation by using NECA as a radioligand |
CHEMBL1125213 |
| ADMET |
k' |
= |
1.29 |
|
Hydrophobicity index |
CHEMBL1125213 |
| Adenosine receptors; A1 & A2 |
Selectivity ratio |
= |
26.0 |
|
It is the ratio of Ki value of A1 receptor to that of A2 receptor. |
CHEMBL1125213 |
| Adenosine A1 receptor |
Ki |
= |
540.0 |
nM |
Binding affinity against adenosine A1 receptor from rat brain. |
CHEMBL1128362 |
| Adenosine A2a receptor |
Ki |
= |
11000.0 |
nM |
Binding affinity against adenosine A2A receptor from rat brain. |
CHEMBL1128362 |
| Adenosine A3 receptor |
Ki |
= |
1330000.0 |
nM |
Binding affinity against adenosine A3 receptor from rat brain. |
CHEMBL1128362 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
0.00041 |
|
Ratio of the binding affinities against rat brain A1 and A3 receptors, KiA1/KiA3. |
CHEMBL1128362 |
| Adenosine receptor A2a and A3 |
Ratio |
= |
0.0083 |
|
Ratio of the binding affinities against rat brain A2a and A3 receptors, KiA2a/KiA3. |
CHEMBL1128362 |
| Adenosine A1 receptor |
Ki |
= |
1081.0 |
nM |
Displacement of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells |
CHEMBL1145202 |
| Adenosine A2a receptor |
Ki |
|
|
nM |
Displacement of [3H]-ZM 241385 binding to human adenosine A2A receptor expressed in CHO cells; nd denotes 'Not determined' |
CHEMBL1145202 |
| Adenosine A3 receptor |
Displacement |
= |
15.0 |
% |
Percent displacement of [125I]AB-MECA binding to human adenosine A3 receptor expressed in HEK 293 cells at 1 uM |
CHEMBL1145202 |
| Adenosine A1 receptor |
Change in cAMP |
= |
72.0 |
% |
Effect on forskolin-induced cAMP levels at human A1 adenosine receptor compared to CPA (full agonist, 100% inhibition) and DPCPX(full inverse agonist, 100% stimulation) |
CHEMBL1145202 |
| Adenosine A1 receptor |
Activity |
|
|
|
Activity at human adenosine A1 receptor expressed in CHO cells assessed as effect on forskolin-stimulated cAMP production at 100 uM |
CHEMBL1141417 |
| Unchecked |
Inhibition |
|
|
% |
Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay |
CHEMBL1255231 |
| Plasmodium falciparum |
IC50 |
= |
6309.57 |
nM |
Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay |
CHEMBL1255382 |
| Nuclear factor NF-kappa-B p105 subunit |
Potency |
= |
398.1 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Identification of Small Molecule Agonists for NFkB Signaling Pathway. (Class of assay: confirmatory) [Related pubchem assays: 895 ] |
CHEMBL1201862 |
| NON-PROTEIN TARGET |
Potency |
= |
3981.1 |
nM |
PUBCHEM_BIOASSAY: qHTS for differential inhibitors of proliferation of Plasmodium falciparum line 3D7. (Class of assay: confirmatory) [Related PubChem assays: 1815 (Assay for Plasmodium falciparum line 7G8), 1816 (Assay for Plasmodium falciparum line GB4), 1828 (Summary assay)] |
CHEMBL1201862 |
| NON-PROTEIN TARGET |
Potency |
= |
11220.2 |
nM |
PUBCHEM_BIOASSAY: qHTS for differential inhibitors of proliferation of Plasmodium falciparum line W2. (Class of assay: confirmatory) [Related PubChem assays: 1815 (Assay for Plasmodium falciparum line 7G8), 1877 (Assay for Plasmodium falciparum line D10), 1816 (Assay for Plasmodium falciparum line GB4), 1876 (Assay for Plasmodium falciparum line 7D3), 1828 (Summary assay)] |
CHEMBL1201862 |
| Peripheral myelin protein 22 |
Potency |
= |
75686.3 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Modulators of Human Peripheral Myelin Protein 22 (PMP22) Expression/Activity. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Pyruvate kinase isozymes M1/M2 |
Potency |
= |
6.3 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Activators of Human Muscle Pyruvate Kinase. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Pyruvate kinase isozymes M1/M2 |
Potency |
= |
6.3 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Human Muscle Pyruvate Kinase. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Nuclear factor NF-kappa-B p105 subunit |
Potency |
= |
398.1 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Identification of Small Molecule Antagonists for NFkB Signaling Pathway. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Anthrax lethal factor |
Potency |
= |
31622.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Anthrax Lethal Toxin Internalization. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Thrombopoietin |
Potency |
= |
10000.0 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Identification of Small Molecule Agonists for Thrombopoietin (TPO) Signaling Pathway. (Class of assay: confirmatory) [Related pubchem assays: 918 ] |
CHEMBL1201862 |
| Cytochrome P450 3A4 |
Potency |
= |
25118.9 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Activators of Cytochrome P450 3A4. (Class of assay: confirmatory) [Related pubchem assays: 410 ] |
CHEMBL1201862 |
| NON-PROTEIN TARGET |
Potency |
= |
10000.0 |
nM |
PUBCHEM_BIOASSAY: qHTS for differential inhibitors of proliferation of Plasmodium falciparum line HB3. (Class of assay: confirmatory) [Related PubChem assays: 1815 (Assay for Plasmodium falciparum line 7G8), 1877 (Assay for Plasmodium falciparum line D10), 1816 (Assay for Plasmodium falciparum line GB4), 1876 (Assay for Plasmodium falciparum line 3D7), 1828 (Summary assay)] |
CHEMBL1201862 |
| Cytochrome P450 2D6 |
Potency |
= |
19952.6 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors and Substrates of Cytochrome P450 2D6. (Class of assay: confirmatory) [Related pubchem assays: 410 ] |
CHEMBL1201862 |
| Cytochrome P450 3A4 |
Potency |
= |
25118.9 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors and Substrates of Cytochrome P450 3A4. (Class of assay: confirmatory) [Related pubchem assays: 410 ] |
CHEMBL1201862 |
| Thrombopoietin |
Potency |
= |
10000.0 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Identification of Small Molecule Antagonists for Thrombopoietin (TPO) Signaling Pathway. (Class of assay: confirmatory) [Related pubchem assays: 917 ] |
CHEMBL1201862 |
| Cytochrome P450 2C9 |
AC50 |
|
|
|
PUBCHEM_BIOASSAY: Cytochrome panel assay with activity outcomes. (Class of assay: other) Panel member name: p450-cyp2c9 Compounds with AC50 equal or less than 10 uM are considered active |
CHEMBL1201862 |
| Cytochrome P450 1A2 |
AC50 |
= |
12589.25 |
nM |
PUBCHEM_BIOASSAY: Cytochrome panel assay with activity outcomes. (Class of assay: other) Panel member name: p450-cyp1a2 Compounds with AC50 equal or less than 10 uM are considered active |
CHEMBL1201862 |
| Cytochrome P450 2D6 |
AC50 |
= |
19952.62 |
nM |
PUBCHEM_BIOASSAY: Cytochrome panel assay with activity outcomes. (Class of assay: other) Panel member name: p450-cyp2d6 Compounds with AC50 equal or less than 10 uM are considered active |
CHEMBL1201862 |
| Cytochrome P450 2C19 |
AC50 |
|
|
|
PUBCHEM_BIOASSAY: Cytochrome panel assay with activity outcomes. (Class of assay: other) Panel member name: p450-cyp2c19 Compounds with AC50 equal or less than 10 uM are considered active |
CHEMBL1201862 |
| Cytochrome P450 3A4 |
AC50 |
= |
25118.86 |
nM |
PUBCHEM_BIOASSAY: Cytochrome panel assay with activity outcomes. (Class of assay: other) Panel member name: p450-cyp3a4 Compounds with AC50 equal or less than 10 uM are considered active |
CHEMBL1201862 |
| DNA polymerase iota |
Potency |
|
3.5 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of Polymerase Iota. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588623] |
CHEMBL1201862 |
| HERG |
Potency |
|
1412.5 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Small Molecule Inhibitors of the Human hERG Channel Activity. (Class of assay: confirmatory) |
CHEMBL1201862 |
