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Assay Detail

CHEMBL660367

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

Functional
Affinity against Cholecystokinin type B receptor expressed in CHO cells on rat brain.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
Bellier B, Million ME, DaNascimento S, Meudal H, Kellou S, Maigret B, Garbay C.
J Med Chem (2000) 43 : 3614 -3623
PubMed 11020275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 8.75 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL262197 1 9.40
CHEMBL120150 1 9.25
CHEMBL1121 SINCALIDE 4.0 1 9.20
CHEMBL64605 1 9.00
CHEMBL120632 TETRAGASTRIN -1.0 1 8.85
CHEMBL100538 1 8.82
CHEMBL333477 1 8.82
CHEMBL331394 1 8.79
CHEMBL321456 1 8.70
CHEMBL120827 1 8.48
CHEMBL411271 1 8.47
CHEMBL177799 1 8.15
CHEMBL408389 1 7.77
CHEMBL120335 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL262197 EC50 = 0.4 nM 9.40
CHEMBL120150 EC50 = 0.56 nM 9.25
CHEMBL1121 SINCALIDE EC50 = 0.63 nM 9.20
CHEMBL64605 EC50 = 1.0 nM 9.00
CHEMBL120632 TETRAGASTRIN EC50 = 1.4 nM 8.85
CHEMBL100538 EC50 = 1.5 nM 8.82
CHEMBL333477 EC50 = 1.5 nM 8.82
CHEMBL331394 EC50 = 1.64 nM 8.79
CHEMBL321456 EC50 = 2.0 nM 8.70
CHEMBL120827 EC50 = 3.3 nM 8.48
CHEMBL411271 EC50 = 3.4 nM 8.47
CHEMBL177799 EC50 = 7.0 nM 8.15
CHEMBL408389 EC50 = 17.0 nM 7.77
CHEMBL120335 EC50 = - nM -