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Assay Detail

CHEMBL1909122

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
DRUGMATRIX: Cannabinoid CB1 radioligand binding (ligand: [3H] SR141716A)
ChEMBL ↗
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Chem-1
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 871 4.85 5.76
Ki 871 4.95 5.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1428 NIMODIPINE 4.0 2 5.86
CHEMBL30008 FLUNARIZINE 2.0 2 5.62
CHEMBL91 MICONAZOLE 4.0 2 4.78
CHEMBL828 PHENOTHIAZINE 2.0 2 4.71
CHEMBL1201151 MESTRANOL 4.0 2 4.65
CHEMBL808 ECONAZOLE 4.0 2 4.54
CHEMBL1909069 — — 2 4.49
CHEMBL264374 BEZAFIBRATE 3.0 2 -
CHEMBL135 ESTRADIOL 4.0 2 -
CHEMBL1077 BROMFENAC 4.0 2 -
CHEMBL894 BUPROPION 4.0 2 -
CHEMBL108 CARBAMAZEPINE 4.0 2 -
CHEMBL24 ATENOLOL 4.0 2 -
CHEMBL1598608 AZASETRON 2.0 2 -
CHEMBL1201346 BALSALAZIDE 4.0 2 -
CHEMBL31184 BENZO[DEF]CHRYSENE 0.5 2 -
CHEMBL113 CAFFEINE 4.0 2 -
CHEMBL1256017 ARCAINE SULFATE — 2 -
CHEMBL415690 BETADEX 3.0 2 -
CHEMBL277474 ANTIPYRINE 3.0 2 -
CHEMBL44814 CARBON TETRACHLORIDE -1.0 2 -
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER — 2 -
CHEMBL221753 BENZETHONIUM CHLORIDE 2.0 2 -
CHEMBL701 BACLOFEN 4.0 2 -
CHEMBL1095699 AZASERINE 2.0 2 -
CHEMBL3084803 ASTROMICIN 2.0 2 -
CHEMBL1200396 BUPIVACAINE HYDROCHLORIDE 4.0 2 -
CHEMBL844 BRIMONIDINE 4.0 2 -
CHEMBL1231530 BETAMIPRON 2.0 2 -
CHEMBL12089 BERBERINE CHLORIDE 1.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1428 NIMODIPINE Ki = 1371.0 nM 5.86
CHEMBL1428 NIMODIPINE IC50 = 1736.0 nM 5.76
CHEMBL30008 FLUNARIZINE Ki = 2391.0 nM 5.62
CHEMBL30008 FLUNARIZINE IC50 = 3028.0 nM 5.52
CHEMBL91 MICONAZOLE Ki = 16614.0 nM 4.78
CHEMBL828 PHENOTHIAZINE Ki = 19624.0 nM 4.71
CHEMBL91 MICONAZOLE IC50 = 21050.0 nM 4.68
CHEMBL1201151 MESTRANOL Ki = 22532.0 nM 4.65
CHEMBL828 PHENOTHIAZINE IC50 = 24857.0 nM 4.61
CHEMBL808 ECONAZOLE Ki = 28627.0 nM 4.54
CHEMBL1201151 MESTRANOL IC50 = 28540.0 nM 4.54
CHEMBL1909069 — Ki = 32470.0 nM 4.49
CHEMBL808 ECONAZOLE IC50 = 36270.0 nM 4.44
CHEMBL1909069 — IC50 = 41129.0 nM 4.39
CHEMBL503 LOVASTATIN IC50 - — -
CHEMBL1373 MODAFINIL Ki - — -
CHEMBL503 LOVASTATIN Ki - — -
CHEMBL1237 LISINOPRIL ANHYDROUS Ki - — -
CHEMBL13 METOPROLOL IC50 - — -
CHEMBL1513 IRBESARTAN IC50 - — -
CHEMBL268291 DIMETHYLFORMAMIDE Ki - — -
CHEMBL268291 DIMETHYLFORMAMIDE IC50 - — -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER Ki - — -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER IC50 - — -
CHEMBL19215 METERGOLINE Ki - — -
CHEMBL19215 METERGOLINE IC50 - — -
CHEMBL45 MELATONIN Ki - — -
CHEMBL45 MELATONIN IC50 - — -
CHEMBL1909068 — Ki - — -
CHEMBL1909068 — IC50 - — -
CHEMBL80 NALOXONE Ki - — -
CHEMBL80 NALOXONE IC50 - — -
CHEMBL1201139 MEGESTROL ACETATE Ki - — -
CHEMBL1373 MODAFINIL IC50 - — -
CHEMBL1201237 LEVOBUNOLOL IC50 - — -
CHEMBL1201237 LEVOBUNOLOL Ki - — -
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 IC50 - — -
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 Ki - — -
CHEMBL1909067 — IC50 - — -
CHEMBL1909067 — Ki - — -
CHEMBL1201139 MEGESTROL ACETATE IC50 - — -
CHEMBL64391 ITRACONAZOLE Ki - — -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE IC50 - — -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE Ki - — -
CHEMBL86 METOCLOPRAMIDE Ki - — -
CHEMBL164290 N-NITROSODIETHYLAMINE IC50 - — -
CHEMBL164290 N-NITROSODIETHYLAMINE Ki - — -
CHEMBL92401 IPRONIAZID IC50 - — -
CHEMBL92401 IPRONIAZID Ki - — -
CHEMBL64391 ITRACONAZOLE IC50 - — -