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Assay Detail

CHEMBL661967

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

Binding
Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cholecystokinin receptor type A (CHEMBL3501)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
Blommaert AG, Dhôtel H, Ducos B, Durieux C, Goudreau N, Bado A, Garbay C, Roques BP.
J Med Chem (1997) 40 : 647 -658
PubMed 9057851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.14 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 9.55
CHEMBL3143501 1 6.57
CHEMBL2371222 1 5.66
CHEMBL2371224 1 5.64
CHEMBL2371221 1 5.61
CHEMBL2371225 1 5.54
CHEMBL120632 TETRAGASTRIN -1.0 1 4.44
CHEMBL2371223 1 -
CHEMBL333477 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE Ki = 0.28 nM 9.55
CHEMBL3143501 Ki = 271.0 nM 6.57
CHEMBL2371222 Ki = 2210.0 nM 5.66
CHEMBL2371224 Ki = 2293.0 nM 5.64
CHEMBL2371221 Ki = 2472.0 nM 5.61
CHEMBL2371225 Ki = 2880.0 nM 5.54
CHEMBL120632 TETRAGASTRIN Ki = 36133.0 nM 4.44
CHEMBL2371223 Ki > 100000.0 nM -
CHEMBL333477 Ki > 5000.0 nM -