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Assay Detail

CHEMBL662562

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

Binding
Displacement of [125I]Bolton-Hunter-CCK-8 from guinea pig cortex Cholecystokinin type B receptor
14
Total Activities
14
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

Toward developing peptidomimetics: Successful replacement of backbone amide bonds in tetrapeptide-based CCK-A receptor agonists
Shiosaki K, Lin CW, Leanna M, Morton HE, Miller TR, Witte D, Stashko M, Nadzan AM
Bioorg Med Chem Lett (1993) 3 : 855 -860
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.04 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1121 SINCALIDE 4.0 1 8.80
CHEMBL64605 1 7.60
CHEMBL169126 1 6.15
CHEMBL171593 1 6.14
CHEMBL355836 1 5.85
CHEMBL422919 1 5.62
CHEMBL436053 1 5.60
CHEMBL435465 1 5.44
CHEMBL354512 1 5.42
CHEMBL171227 1 5.35
CHEMBL354171 1 5.30
CHEMBL263525 1 5.16
CHEMBL354670 1 -
CHEMBL169567 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1121 SINCALIDE IC50 = 1.6 nM 8.80
CHEMBL64605 IC50 = 25.0 nM 7.60
CHEMBL169126 IC50 = 710.0 nM 6.15
CHEMBL171593 IC50 = 730.0 nM 6.14
CHEMBL355836 IC50 = 1400.0 nM 5.85
CHEMBL422919 IC50 = 2400.0 nM 5.62
CHEMBL436053 IC50 = 2500.0 nM 5.60
CHEMBL435465 IC50 = 3600.0 nM 5.44
CHEMBL354512 IC50 = 3800.0 nM 5.42
CHEMBL171227 IC50 = 4500.0 nM 5.35
CHEMBL354171 IC50 = 5000.0 nM 5.30
CHEMBL263525 IC50 = 7000.0 nM 5.16
CHEMBL354670 IC50 > 10000.0 nM -
CHEMBL169567 IC50 > 10000.0 nM -