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Assay Detail

CHEMBL656925

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

Binding
Affinity to inhibit [3H]pCCK-8 specific binding on rat brain Cholecystokinin type B receptor expressed in CHO cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastrin/cholecystokinin type B receptor (CHEMBL3508)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 7 7.52 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 9.22
CHEMBL2371222 1 7.75
CHEMBL2371221 1 7.64
CHEMBL3143501 1 7.10
CHEMBL333477 1 7.06
CHEMBL120632 TETRAGASTRIN -1.0 1 7.03
CHEMBL2371225 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE Ki = 0.6 nM 9.22
CHEMBL2371222 Ki = 18.0 nM 7.75
CHEMBL2371221 Ki = 23.0 nM 7.64
CHEMBL3143501 Ki = 80.0 nM 7.10
CHEMBL333477 Ki = 87.0 nM 7.06
CHEMBL120632 TETRAGASTRIN Ki = 93.0 nM 7.03
CHEMBL2371225 Ki = 142.0 nM 6.85