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Assay Detail

CHEMBL662569

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

Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type B receptor in guinea pig cortex
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Gastrin/cholecystokinin type B receptor (CHEMBL298)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists
Showell GA, Bourrain S, Fletcher SR, Neduvelil JG, Fletcher AE, Freedman SB, Patel S, Smith AJ, Marshall GR, Graham MI, Sohal B, Matassa VG
Bioorg Med Chem Lett (1995) 5 : 3023 -3026
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.81 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420783 L-740093 1 10.00
CHEMBL103119 1 8.74
CHEMBL102633 1 8.31
CHEMBL9387 L-365260 1 8.07
CHEMBL101528 1 8.01
CHEMBL105273 1 7.93
CHEMBL100502 1 7.74
CHEMBL103791 1 7.51
CHEMBL103229 1 6.92
CHEMBL319180 1 6.57
CHEMBL102537 1 6.06
CHEMBL431832 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420783 L-740093 IC50 = 0.1 nM 10.00
CHEMBL103119 IC50 = 1.81 nM 8.74
CHEMBL102633 IC50 = 4.9 nM 8.31
CHEMBL9387 L-365260 IC50 = 8.5 nM 8.07
CHEMBL101528 IC50 = 9.8 nM 8.01
CHEMBL105273 IC50 = 11.8 nM 7.93
CHEMBL100502 IC50 = 18.3 nM 7.74
CHEMBL103791 IC50 = 31.0 nM 7.51
CHEMBL103229 IC50 = 121.0 nM 6.92
CHEMBL319180 IC50 = 270.0 nM 6.57
CHEMBL102537 IC50 = 880.0 nM 6.06
CHEMBL431832 IC50 > 3000.0 nM -