| Rattus norvegicus |
IC50 |
= |
17.0 |
nM |
In vitro inhibition of synaptic potential in the hippocampal formation (synaptic responses (fEPSPs) recorded in the CAI region of in vivo hippocampal slices in rat brain) |
CHEMBL1125345 |
| Adenosine A1 receptor |
Ki |
= |
0.85 |
nM |
Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor |
CHEMBL1125345 |
| Adenosine A1 receptor |
Ki |
= |
0.85 |
nM |
Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand |
CHEMBL1125572 |
| Adenosine A2 receptor |
Ratio |
= |
210.0 |
nM |
Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand |
CHEMBL1125572 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
250.0 |
|
Ratio of A2 to A1. |
CHEMBL1125572 |
| Adenosine A1 receptor |
Ki |
= |
1.3 |
nM |
Affinity for adenosine A1 receptor using [3H]N6-(phenylisopropyl)adenosine (R)-[3H]-PIA as a radioligand in rat brain. |
CHEMBL1124458 |
| Adenosine A1 receptor |
Ki |
|
|
nM |
Displacement of [3H]-N6 -(phenylisopropyl)-adenosine (R)-[3H]-PIA from Adenosine A1 receptor of calf brain |
CHEMBL1124458 |
| Adenosine A1 receptor |
Inhibition |
|
|
% |
Inhibition of [125I]APNEA binding to adenosine A1 receptor of rat brain |
CHEMBL1124458 |
| Adenosine A1 receptor |
Ki |
= |
0.85 |
nM |
Inhibition of binding of 1 nM N6-[3H]cyclohexyladenosine to adenosine A1 receptor on rat cerebral cortical membranes. |
CHEMBL1123049 |
| Beta-lactamase AmpC |
Potency |
= |
63095.7 |
nM |
PUBCHEM_BIOASSAY: qHTS Inhibitors of AmpC Beta-Lactamase (assay with detergent). (Class of assay: confirmatory) [Related pubchem assays: 1002 (Confirmation Concentration-Response Assay for Inhibitors of AmpC Beta-Lactamase (assay with detergent)), 585 (Promiscuous and Specific Inhibitors of AmpC Beta-Lactamase (assay without detergent) - a screen old NIH MLSMR collection), 584 (Promiscuous and Specific Inhibitors of AmpC Beta-Lactamase (assay with detergent) - a screen of the old NIH MLSMR collection), 1003 (Confirmation Cuvette-Based Assay for Inhibitors of AmpC Beta-Lactamase (assay with detergent))] |
CHEMBL1201862 |
| Relaxin receptor 1 |
Potency |
= |
1412.5 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Relaxin receptor 2 |
Potency |
|
6897.0 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP2 Hit Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2676, AID2703, AID489012] |
CHEMBL1201862 |
| Relaxin receptor 1 |
Potency |
|
1226.5 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP1 Hit Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2676, AID2703, AID489043, AID492948] |
CHEMBL1201862 |
| Unchecked |
Potency |
|
163.6 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay to Find Inhibitors of Chronic Active B-Cell Receptor Signaling. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485345, AID485355] |
CHEMBL1201862 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
326.3 |
nM |
PUBCHEM_BIOASSAY: qHTS 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):AID493106, AID493143] |
CHEMBL1201862 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Potency |
|
31622.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Histone Lysine Methyltransferase G9a. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504404] |
CHEMBL1201862 |
| Vasopressin V1b receptor |
Potency |
|
2745.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1: V1B Hit Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2676, AID2703, AID489012] |
CHEMBL1201862 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
25118.9 |
nM |
PUBCHEM_BIOASSAY: qHTS 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):AID493107, AID493125] |
CHEMBL1201862 |
| Runt-related transcription factor 1/Core-binding factor subunit beta |
Potency |
|
31622.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Compounds Blocking the Interaction Between CBF-beta and RUNX1 for the Treatment of Acute Myeloid Leukemia. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID1484, AID504370, AID504374, AID504375] |
CHEMBL1201862 |
| DNA polymerase iota |
Potency |
|
89125.1 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of Polymerase Iota. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588623] |
CHEMBL1201862 |
| Regulator of G-protein signaling 4 |
Potency |
|
50118.7 |
nM |
PUBCHEM_BIOASSAY: Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504856] |
CHEMBL1201862 |
| Flap endonuclease 1 |
Potency |
|
70794.6 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for the Inhibitors of Human Flap endonuclease 1 (FEN1). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488813] |
CHEMBL1201862 |
| HepG2 |
Potency |
|
35481.3 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of TGF-b: Cytotox Counterscreen. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588855, AID588860] |
CHEMBL1201862 |
| Luciferin 4-monooxygenase |
Potency |
|
30131.3 |
nM |
PUBCHEM_BIOASSAY: qHTS profiling assay for firefly luciferase inhibitor/activator using purified enzyme and Km concentrations of substrates (counterscreen for miR-21 project). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2288, AID2289, AID2598, AID411] |
CHEMBL1201862 |
| Relaxin receptor 1 |
Potency |
|
19438.4 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1: THP1 Hit Validation. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Geminin |
Potency |
|
501.2 |
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 |
| Unchecked |
Potency |
|
461.1 |
nM |
PubChem BioAssay. qHTS Assay to Find Inhibitors of Chronic Active B-Cell Receptor Signaling: Hit Validation in Primary Screen. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Mus musculus |
Activity |
|
|
|
Anticonvulsant activity in CF-1 albino mouse assessed as protection against subcutaneous metrazol-induced seizures at 1 mg/kg, ip |
CHEMBL2169760 |
| Mus musculus |
Activity |
|
|
|
Anticonvulsant activity in CF-1 albino mouse assessed as protection against subcutaneous metrazol-induced seizures at 3 mg/kg, ip |
CHEMBL2169760 |
| Mus musculus |
Activity |
|
|
|
Anticonvulsant activity in CF-1 albino mouse assessed as protection against maximal electroshock-induced seizures at 2 mg/kg, ip by MES test |
CHEMBL2169760 |
| Mus musculus |
Activity |
|
|
|
Anticonvulsant activity in CF-1 albino mouse assessed as protection against maximal electroshock-induced seizures at 1 mg/kg, ip by MES test |
CHEMBL2169760 |
| Mus musculus |
Activity |
|
|
|
Anticonvulsant activity in CF-1 albino mouse assessed as protection against maximal electroshock-induced seizures at 3 mg/kg, ip by MES test |
CHEMBL2169760 |
| Mus musculus |
ED50 |
= |
0.03 |
mg.kg-1 |
Anticonvulsant activity in ip dosed CF-1 albino mouse assessed as protection against 6 Hz psychomotor seizure after 1 hr by minimal clonic seizure test |
CHEMBL2169760 |
| Mus musculus |
TD50 |
= |
0.14 |
mg kg-1 |
Toxicity in ip dosed CF-1 albino mouse assessed as behavioral changes after 4 hrs by rotarod test |
CHEMBL2169760 |
| Adenosine A1 receptor |
Inhibition |
= |
94.0 |
% |
Activity at human A1 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 10 uM after 30 min |
CHEMBL2169760 |
| Adenosine A3 receptor |
Ki |
= |
12.4 |
nM |
Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cells after 60 min Packard Cobra 2 gamma-counter |
CHEMBL2169760 |
| Adenosine A2a receptor |
Ki |
= |
370.0 |
nM |
Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer |
CHEMBL2169760 |
| Adenosine A1 receptor |
Ki |
= |
10.4 |
nM |
Displacement of [3H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer |
CHEMBL2169760 |
| DNA-(apurinic or apyrimidinic site) lyase |
Potency |
|
354.8 |
nM |
PubChem BioAssay. qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1). (Class of assay: confirmatory) |
CHEMBL1201862 |
