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Assay Detail

CHEMBL657475

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

Binding
Tested for its activity to inhibit the binding of [125I]CCK-33 to Cholecystokinin type B receptor in guinea pig brain
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Gastrin/cholecystokinin type B receptor (CHEMBL298)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Multipurpose receptor ligands: -carboline cholecystokinin antagonists
Evans BE, Rittle KE, Chang RS, Lotti VJ, Freedman SB, Freidinger RM
Bioorg Med Chem Lett (1993) 3 : 867 -870
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.23 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169661 1 8.26
CHEMBL354802 1 6.57
CHEMBL355092 1 6.39
CHEMBL352573 1 5.23
CHEMBL354126 1 4.96
CHEMBL71079 1 4.82
CHEMBL171108 1 4.47
CHEMBL72073 1 4.40
CHEMBL353304 1 4.17
CHEMBL169675 1 4.17
CHEMBL353088 1 4.14
CHEMBL453066 BETA-CCM 1 -
CHEMBL171940 1 -
CHEMBL169767 1 -
CHEMBL54381 1 -
CHEMBL171651 1 -
CHEMBL169953 1 -
CHEMBL171531 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169661 IC50 = 5.5 nM 8.26
CHEMBL354802 IC50 = 270.0 nM 6.57
CHEMBL355092 IC50 = 410.0 nM 6.39
CHEMBL352573 IC50 = 5900.0 nM 5.23
CHEMBL354126 IC50 = 11000.0 nM 4.96
CHEMBL71079 IC50 = 15000.0 nM 4.82
CHEMBL171108 IC50 = 34000.0 nM 4.47
CHEMBL72073 IC50 = 40000.0 nM 4.40
CHEMBL353304 IC50 = 67000.0 nM 4.17
CHEMBL169675 IC50 = 68000.0 nM 4.17
CHEMBL353088 IC50 = 72000.0 nM 4.14
CHEMBL453066 BETA-CCM IC50 > 100000.0 nM -
CHEMBL171940 IC50 = 223000.0 nM -
CHEMBL169767 IC50 > 100000.0 nM -
CHEMBL54381 IC50 > 100000.0 nM -
CHEMBL171651 IC50 > 100000.0 nM -
CHEMBL169953 IC50 > 100000.0 nM -
CHEMBL171531 IC50 > 100000.0 nM -