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Assay Detail

CHEMBL662405

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

Binding
In vitro inhibition of [3H]propionyl-CCK-8 binding to rat pancreatic membranes at Cholecystokinin type A receptor.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.
Martín-Martínez M, De La Figuera N, Latorre M, Herranz R, García-López MT, Cenarruzabeitia E, Del Río J, González-Muñiz R.
J Med Chem (2000) 43 : 3770 -3777
PubMed 11020292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.71 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9506 DEVAZEPIDE 2.0 1 9.15
CHEMBL13577 1 8.76
CHEMBL276837 1 8.33
CHEMBL419237 1 8.13
CHEMBL126160 1 7.32
CHEMBL124798 1 7.26
CHEMBL331532 1 7.06
CHEMBL262463 1 7.01
CHEMBL338186 1 6.35
CHEMBL273543 1 -
CHEMBL337988 1 -
CHEMBL435407 1 -
CHEMBL125897 1 -
CHEMBL124491 1 -
CHEMBL338656 1 -
CHEMBL421461 1 -
CHEMBL338146 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9506 DEVAZEPIDE IC50 = 0.71 nM 9.15
CHEMBL13577 IC50 = 1.73 nM 8.76
CHEMBL276837 IC50 = 4.7 nM 8.33
CHEMBL419237 IC50 = 7.4 nM 8.13
CHEMBL126160 IC50 = 47.5 nM 7.32
CHEMBL124798 IC50 = 54.6 nM 7.26
CHEMBL331532 IC50 = 88.0 nM 7.06
CHEMBL262463 IC50 = 97.8 nM 7.01
CHEMBL338186 IC50 = 450.0 nM 6.35
CHEMBL273543 IC50 > 1000.0 nM -
CHEMBL337988 IC50 > 1000.0 nM -
CHEMBL435407 IC50 > 1000.0 nM -
CHEMBL125897 IC50 > 1000.0 nM -
CHEMBL124491 IC50 > 1000.0 nM -
CHEMBL338656 IC50 > 1000.0 nM -
CHEMBL421461 IC50 > 1000.0 nM -
CHEMBL338146 IC50 > 1000.0 nM -