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Assay Detail

CHEMBL1909124

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

Binding
DRUGMATRIX: Chemokine CCR2B radioligand binding (ligand: [125I] MCP-1)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 2 (CHEMBL4015)
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 5.31 5.66
Ki 871 5.72 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193 NIFEDIPINE 4.0 2 6.07
CHEMBL508112 BENZOTHIAZYL DISULFIDE 2 6.03
CHEMBL964 DISULFIRAM 4.0 2 6.02
CHEMBL270299 BAY-11-7085 2 5.79
CHEMBL1381098 1-NAPHTHYLISOTHIOCYANATE 2 5.59
CHEMBL633 AMIODARONE 4.0 2 5.37
CHEMBL11359 CISPLATIN 4.0 2 5.15
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
CHEMBL193 NIFEDIPINE Ki = 847.0 nM 6.07
CHEMBL508112 BENZOTHIAZYL DISULFIDE Ki = 929.0 nM 6.03
CHEMBL964 DISULFIRAM Ki = 954.0 nM 6.02
CHEMBL270299 BAY-11-7085 Ki = 1614.0 nM 5.79
CHEMBL193 NIFEDIPINE IC50 = 2191.0 nM 5.66
CHEMBL508112 BENZOTHIAZYL DISULFIDE IC50 = 2405.0 nM 5.62
CHEMBL964 DISULFIRAM IC50 = 2468.0 nM 5.61
CHEMBL1381098 1-NAPHTHYLISOTHIOCYANATE Ki = 2589.0 nM 5.59
CHEMBL270299 BAY-11-7085 IC50 = 4177.0 nM 5.38
CHEMBL633 AMIODARONE Ki = 4285.0 nM 5.37
CHEMBL1381098 1-NAPHTHYLISOTHIOCYANATE IC50 = 6699.0 nM 5.17
CHEMBL11359 CISPLATIN Ki = 7012.0 nM 5.15
CHEMBL633 AMIODARONE IC50 = 11086.0 nM 4.96
CHEMBL11359 CISPLATIN IC50 = 18142.0 nM 4.74
CHEMBL164290 N-NITROSODIETHYLAMINE Ki - -
CHEMBL45 MELATONIN IC50 - -
CHEMBL92401 IPRONIAZID IC50 - -
CHEMBL92401 IPRONIAZID Ki - -
CHEMBL64391 ITRACONAZOLE IC50 - -
CHEMBL64391 ITRACONAZOLE Ki - -
CHEMBL1909068 Ki - -
CHEMBL480 LANSOPRAZOLE Ki - -
CHEMBL1201193 LEVOBUPIVACAINE IC50 - -
CHEMBL1201193 LEVOBUPIVACAINE Ki - -
CHEMBL1237 LISINOPRIL ANHYDROUS IC50 - -
CHEMBL1237 LISINOPRIL ANHYDROUS Ki - -
CHEMBL1909068 IC50 - -
CHEMBL19215 METERGOLINE IC50 - -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER IC50 - -
CHEMBL19215 METERGOLINE Ki - -
CHEMBL480 LANSOPRAZOLE IC50 - -
CHEMBL45 MELATONIN Ki - -
CHEMBL1909067 Ki - -
CHEMBL741 LAMOTRIGINE IC50 - -
CHEMBL6437 MIANSERIN Ki - -
CHEMBL741 LAMOTRIGINE Ki - -
CHEMBL1201237 LEVOBUNOLOL IC50 - -
CHEMBL1201237 LEVOBUNOLOL Ki - -
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 IC50 - -
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 Ki - -
CHEMBL1909067 IC50 - -
CHEMBL164290 N-NITROSODIETHYLAMINE IC50 - -
CHEMBL1201139 MEGESTROL ACETATE IC50 - -
CHEMBL1201139 MEGESTROL ACETATE Ki - -
CHEMBL1201151 MESTRANOL IC50 - -
CHEMBL1201151 MESTRANOL Ki - -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE IC50 - -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE Ki - -
CHEMBL86 METOCLOPRAMIDE IC50 - -
CHEMBL86 METOCLOPRAMIDE Ki - -