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Assay Detail

CHEMBL1909149

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

Binding
DRUGMATRIX: GABAA, Chloride Channel, TBOB radioligand binding (ligand: [3H] TBOB)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.47
Ki 871 5.36 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873703 DIELDRIN 2.0 2 6.52
CHEMBL47244 PICROTOXININ 2 6.48
CHEMBL411 DIETHYLSTILBESTROL 4.0 2 4.87
CHEMBL160 CYCLOSPORINE 4.0 2 4.87
CHEMBL104 CLOTRIMAZOLE 4.0 2 4.77
CHEMBL103 PROGESTERONE 4.0 2 4.65
CHEMBL1077 BROMFENAC 4.0 2 -
CHEMBL253376 BROMHEXINE 3.0 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 -
CHEMBL108 CARBAMAZEPINE 4.0 2 -
CHEMBL402794 BIS(2-ETHYLHEXYL)PHTHALATE 2 -
CHEMBL264374 BEZAFIBRATE 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 -
CHEMBL1231530 BETAMIPRON 2.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873703 DIELDRIN Ki = 300.0 nM 6.52
CHEMBL47244 PICROTOXININ Ki = 330.0 nM 6.48
CHEMBL1873703 DIELDRIN IC50 = 335.0 nM 6.47
CHEMBL47244 PICROTOXININ IC50 = 368.0 nM 6.43
CHEMBL411 DIETHYLSTILBESTROL Ki = 13529.0 nM 4.87
CHEMBL160 CYCLOSPORINE Ki = 13358.0 nM 4.87
CHEMBL160 CYCLOSPORINE IC50 = 14899.0 nM 4.83
CHEMBL411 DIETHYLSTILBESTROL IC50 = 15090.0 nM 4.82
CHEMBL104 CLOTRIMAZOLE Ki = 16811.0 nM 4.77
CHEMBL104 CLOTRIMAZOLE IC50 = 18751.0 nM 4.73
CHEMBL103 PROGESTERONE Ki = 22289.0 nM 4.65
CHEMBL103 PROGESTERONE IC50 = 24861.0 nM 4.60
CHEMBL2106399 KITASAMYCIN IC50 - -
CHEMBL19019 NALTREXONE Ki - -
CHEMBL2106399 KITASAMYCIN Ki - -
CHEMBL503 LOVASTATIN IC50 - -
CHEMBL503 LOVASTATIN Ki - -
CHEMBL1201193 LEVOBUPIVACAINE IC50 - -
CHEMBL1513 IRBESARTAN IC50 - -
CHEMBL80 NALOXONE Ki - -
CHEMBL80 NALOXONE IC50 - -
CHEMBL878 METOLAZONE Ki - -
CHEMBL878 METOLAZONE IC50 - -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER Ki - -
CHEMBL313493 METHANESULFONIC ACID METHYL ESTER IC50 - -
CHEMBL19215 METERGOLINE Ki - -
CHEMBL19215 METERGOLINE IC50 - -
CHEMBL1237 LISINOPRIL ANHYDROUS Ki - -
CHEMBL1237 LISINOPRIL ANHYDROUS IC50 - -
CHEMBL1201193 LEVOBUPIVACAINE Ki - -
CHEMBL1201139 MEGESTROL ACETATE Ki - -
CHEMBL86 METOCLOPRAMIDE IC50 - -
CHEMBL91 MICONAZOLE Ki - -
CHEMBL1201237 LEVOBUNOLOL IC50 - -
CHEMBL1201237 LEVOBUNOLOL Ki - -
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 IC50 - -
CHEMBL1909064 LIPOPOLYSACCHARIDE E. COLI O55:B5 Ki - -
CHEMBL1201151 MESTRANOL IC50 - -
CHEMBL1201151 MESTRANOL Ki - -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE IC50 - -
CHEMBL1354199 METHSCOPOLAMINE BROMIDE Ki - -
CHEMBL64391 ITRACONAZOLE Ki - -
CHEMBL86 METOCLOPRAMIDE Ki - -
CHEMBL6437 MIANSERIN IC50 - -
CHEMBL6437 MIANSERIN Ki - -
CHEMBL1618305 NALOXONAZINE IC50 - -
CHEMBL1618305 NALOXONAZINE Ki - -
CHEMBL92401 IPRONIAZID IC50 - -
CHEMBL92401 IPRONIAZID Ki - -
CHEMBL64391 ITRACONAZOLE IC50 - -