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Assay Detail

CHEMBL662425

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

Binding
Inhibition of [125 I]BH CCK-8S binding to Cholecystokinin type A receptor in pancreatic tissue
12
Total Activities
12
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

Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.
Castro JL, Ball RG, Broughton HB, Russell MG, Rathbone D, Watt AP, Baker R, Chapman KL, Fletcher AE, Patel S, Smith AJ, Marshall GR, Ryecroft W, Matassa VG.
J Med Chem (1996) 39 : 842 -849
PubMed 8632408 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.91 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2110202 1 6.82
CHEMBL168263 1 6.70
CHEMBL2093059 1 6.40
CHEMBL9387 L-365260 1 6.13
CHEMBL2110201 1 6.10
CHEMBL168253 1 5.80
CHEMBL170275 1 5.52
CHEMBL169362 1 5.52
CHEMBL168903 1 5.52
CHEMBL353509 1 5.52
CHEMBL22003 1 5.52
CHEMBL166941 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2110202 IC50 = 153.0 nM 6.82
CHEMBL168263 IC50 = 200.0 nM 6.70
CHEMBL2093059 IC50 = 400.0 nM 6.40
CHEMBL9387 L-365260 IC50 = 736.0 nM 6.13
CHEMBL2110201 IC50 = 802.0 nM 6.10
CHEMBL168253 IC50 = 1600.0 nM 5.80
CHEMBL170275 IC50 = 3000.0 nM 5.52
CHEMBL169362 IC50 = 3000.0 nM 5.52
CHEMBL168903 IC50 = 3000.0 nM 5.52
CHEMBL353509 IC50 = 3000.0 nM 5.52
CHEMBL22003 IC50 = 3000.0 nM 5.52
CHEMBL166941 IC50 = 4080.0 nM 5.39