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Assay Detail

CHEMBL1909166

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

Binding
DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Melanocortin receptor 3 (CHEMBL4644)
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 5.02 6.71
Ki 871 5.08 6.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6067481 COLISTIN 4.0 2 6.78
CHEMBL1221512 2 5.53
CHEMBL633 AMIODARONE 4.0 2 4.97
CHEMBL296419 ASTEMIZOLE 4.0 2 4.87
CHEMBL141343 2 4.82
CHEMBL91 MICONAZOLE 4.0 2 4.79
CHEMBL83 TAMOXIFEN 4.0 2 4.76
CHEMBL71 CHLORPROMAZINE 4.0 2 4.67
CHEMBL808 ECONAZOLE 4.0 2 4.50
CHEMBL1231530 BETAMIPRON 2.0 2 -
CHEMBL1077 BROMFENAC 4.0 2 -
CHEMBL894 BUPROPION 4.0 2 -
CHEMBL319244 CAFFEIC ACID PHENETHYL ESTER 2 -
CHEMBL277474 ANTIPYRINE 3.0 2 -
CHEMBL24 ATENOLOL 4.0 2 -
CHEMBL1598608 AZASETRON 2.0 2 -
CHEMBL1201346 BALSALAZIDE 4.0 2 -
CHEMBL31184 BENZO[DEF]CHRYSENE 0.5 2 -
CHEMBL415690 BETADEX 3.0 2 -
CHEMBL12089 BERBERINE CHLORIDE 1.0 2 -
CHEMBL221753 BENZETHONIUM CHLORIDE 2.0 2 -
CHEMBL701 BACLOFEN 4.0 2 -
CHEMBL1095699 AZASERINE 2.0 2 -
CHEMBL3084803 ASTROMICIN 2.0 2 -
CHEMBL211501 ANTIMYCIN A 2 -
CHEMBL14 CARBACHOL 4.0 2 -
CHEMBL1458880 CADMIUM DICHLORIDE 2 -
CHEMBL1200396 BUPIVACAINE HYDROCHLORIDE 4.0 2 -
CHEMBL844 BRIMONIDINE 4.0 2 -
CHEMBL388590 BENZBROMARONE 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6067481 COLISTIN Ki = 168.0 nM 6.78
CHEMBL6067481 COLISTIN IC50 = 193.0 nM 6.71
CHEMBL1221512 Ki = 2963.0 nM 5.53
CHEMBL1221512 IC50 = 3395.0 nM 5.47
CHEMBL633 AMIODARONE Ki = 10797.0 nM 4.97
CHEMBL633 AMIODARONE IC50 = 12372.0 nM 4.91
CHEMBL296419 ASTEMIZOLE Ki = 13549.0 nM 4.87
CHEMBL141343 Ki = 15102.0 nM 4.82
CHEMBL296419 ASTEMIZOLE IC50 = 15525.0 nM 4.81
CHEMBL91 MICONAZOLE Ki = 16132.0 nM 4.79
CHEMBL141343 IC50 = 17304.0 nM 4.76
CHEMBL83 TAMOXIFEN Ki = 17329.0 nM 4.76
CHEMBL91 MICONAZOLE IC50 = 18485.0 nM 4.73
CHEMBL83 TAMOXIFEN IC50 = 19856.0 nM 4.70
CHEMBL71 CHLORPROMAZINE Ki = 21244.0 nM 4.67
CHEMBL71 CHLORPROMAZINE IC50 = 24343.0 nM 4.61
CHEMBL808 ECONAZOLE Ki = 31426.0 nM 4.50
CHEMBL808 ECONAZOLE IC50 = 36009.0 nM 4.44
CHEMBL1201237 LEVOBUNOLOL Ki - -
CHEMBL1201151 MESTRANOL IC50 - -
CHEMBL1201151 MESTRANOL Ki - -
CHEMBL1373 MODAFINIL IC50 - -
CHEMBL1373 MODAFINIL Ki - -
CHEMBL164290 N-NITROSODIETHYLAMINE IC50 - -
CHEMBL164290 N-NITROSODIETHYLAMINE Ki - -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER IC50 - -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER Ki - -
CHEMBL878 METOLAZONE IC50 - -
CHEMBL878 METOLAZONE Ki - -
CHEMBL80 NALOXONE IC50 - -
CHEMBL80 NALOXONE Ki - -
CHEMBL1513 IRBESARTAN IC50 - -
CHEMBL1201139 MEGESTROL ACETATE Ki - -
CHEMBL64391 ITRACONAZOLE Ki - -
CHEMBL64391 ITRACONAZOLE IC50 - -
CHEMBL92401 IPRONIAZID Ki - -
CHEMBL92401 IPRONIAZID IC50 - -
CHEMBL1618305 NALOXONAZINE Ki - -
CHEMBL1618305 NALOXONAZINE IC50 - -
CHEMBL6437 MIANSERIN Ki - -
CHEMBL6437 MIANSERIN IC50 - -
CHEMBL86 METOCLOPRAMIDE Ki - -
CHEMBL86 METOCLOPRAMIDE IC50 - -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE Ki - -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE IC50 - -
CHEMBL19019 NALTREXONE Ki - -
CHEMBL19019 NALTREXONE IC50 - -
CHEMBL1630579 MYRTECAINE Ki - -
CHEMBL1630579 MYRTECAINE IC50 - -
CHEMBL741 LAMOTRIGINE IC50 - -