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Assay Detail

CHEMBL662420

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

Binding
Displacement of [125I]-BH CCK-8S from Cholecystokinin type A receptor in rat pancreas
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cholecystokinin receptor type A (CHEMBL2871)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 13 5.63 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9387 L-365260 1 6.13
CHEMBL103119 1 5.81
CHEMBL420783 L-740093 1 5.79
CHEMBL319180 1 5.72
CHEMBL101528 1 5.50
CHEMBL105273 1 5.42
CHEMBL103229 1 5.37
CHEMBL100502 1 5.28
CHEMBL102633 1 -
CHEMBL102537 1 -
CHEMBL431832 1 -
CHEMBL103791 1 -
CHEMBL318360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9387 L-365260 IC50 = 736.0 nM 6.13
CHEMBL103119 IC50 = 1559.0 nM 5.81
CHEMBL420783 L-740093 IC50 = 1604.0 nM 5.79
CHEMBL319180 IC50 = 1900.0 nM 5.72
CHEMBL101528 IC50 = 3200.0 nM 5.50
CHEMBL105273 IC50 = 3800.0 nM 5.42
CHEMBL103229 IC50 = 4257.0 nM 5.37
CHEMBL100502 IC50 = 5310.0 nM 5.28
CHEMBL102633 IC50 > 3000.0 nM -
CHEMBL102537 IC50 > 3000.0 nM -
CHEMBL431832 IC50 > 3000.0 nM -
CHEMBL103791 IC50 > 3000.0 nM -
CHEMBL318360 IC50 > 3000.0 nM -