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Assay Detail

CHEMBL662233

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

Binding
Half maximal inhibition of specific binding of [125I]-Bolton-Hunter CCK-8 to Cholecystokinin type A receptor in the rat pancreas
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Development of peptide 3D structure mimetics: rational design of novel peptoid cholecystokinin receptor antagonists.
Low CM, Black JW, Broughton HB, Buck IM, Davies JM, Dunstone DJ, Hull RA, Kalindjian SB, McDonald IM, Pether MJ, Shankley NP, Steel KI.
J Med Chem (2000) 43 : 3505 -3517
PubMed 11000005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.41 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9506 DEVAZEPIDE 2.0 1 10.10
CHEMBL420320 1 8.55
CHEMBL70380 1 8.52
CHEMBL419764 1 8.08
CHEMBL138534 1 7.59
CHEMBL9387 L-365260 1 6.55
CHEMBL117281 1 5.19
CHEMBL333081 1 4.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9506 DEVAZEPIDE IC50 = 0.08 nM 10.10
CHEMBL420320 IC50 = 2.8 nM 8.55
CHEMBL70380 IC50 = 3.0 nM 8.52
CHEMBL419764 IC50 = 8.3 nM 8.08
CHEMBL138534 IC50 = 25.5 nM 7.59
CHEMBL9387 L-365260 IC50 = 280.0 nM 6.55
CHEMBL117281 IC50 = 6400.0 nM 5.19
CHEMBL333081 IC50 = 20500.0 nM 4.69