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Assay Detail

CHEMBL653051

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

Binding
In vitro binding affinity at benzodiazepine receptor of rat cerebral cortical membranes by [3H]diazepam displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Allen MS, LaLoggia AJ, Dorn LJ, Martin MJ, Costantino G, Hagen TJ, Koehler KF, Skolnick P, Cook JM.
J Med Chem (1992) 35 : 4001 -4010
PubMed 1331452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.21 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69719 1 8.55
CHEMBL11709 1 8.30
CHEMBL453066 BETA-CCM 1 8.30
CHEMBL307783 1 8.00
CHEMBL52750 1 7.96
CHEMBL299250 1 7.62
CHEMBL1269093 1 7.03
CHEMBL66902 1 7.01
CHEMBL128348 1 6.98
CHEMBL54228 1 6.91
CHEMBL129742 1 6.45
CHEMBL86231 1 6.33
CHEMBL67421 1 6.30
CHEMBL87641 1 6.27
CHEMBL67951 1 6.12
CHEMBL56459 1 -
CHEMBL87331 1 -
CHEMBL54381 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69719 IC50 = 2.8 nM 8.55
CHEMBL11709 IC50 = 5.0 nM 8.30
CHEMBL453066 BETA-CCM IC50 = 5.0 nM 8.30
CHEMBL307783 IC50 = 10.0 nM 8.00
CHEMBL52750 IC50 = 11.0 nM 7.96
CHEMBL299250 IC50 = 24.0 nM 7.62
CHEMBL1269093 IC50 = 93.0 nM 7.03
CHEMBL66902 IC50 = 98.0 nM 7.01
CHEMBL128348 IC50 = 104.0 nM 6.98
CHEMBL54228 IC50 = 124.0 nM 6.91
CHEMBL129742 IC50 = 358.0 nM 6.45
CHEMBL86231 IC50 = 471.0 nM 6.33
CHEMBL67421 IC50 = 500.0 nM 6.30
CHEMBL87641 IC50 = 535.0 nM 6.27
CHEMBL67951 IC50 = 750.0 nM 6.12
CHEMBL56459 IC50 > 1280.0 nM -
CHEMBL87331 IC50 > 1000.0 nM -
CHEMBL54381 IC50 > 25000.0 nM -