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Assay Detail

CHEMBL661825

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

Binding
Binding affinity for Cholecystokinin type A receptor in guinea pig pancreas by using [125I]BH-CCK-8 as radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cholecystokinin receptor type A (CHEMBL3501)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.
Shiosaki K, Lin CW, Kopecka H, Tufano MD, Bianchi BR, Miller TR, Witte DG, Nadzan AM.
J Med Chem (1991) 34 : 2837 -2842
PubMed 1716682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.23 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3142695 1 8.44
CHEMBL320868 1 8.42
CHEMBL319340 1 8.42
CHEMBL3142693 1 8.10
CHEMBL3142705 1 7.80
CHEMBL3142683 1 7.80
CHEMBL3142682 1 7.68
CHEMBL3142903 1 7.66
CHEMBL3142694 1 7.64
CHEMBL100609 1 7.64
CHEMBL3142906 1 7.47
CHEMBL3142692 1 7.29
CHEMBL3142696 1 7.23
CHEMBL3142697 1 7.22
CHEMBL3142681 1 7.03
CHEMBL3142702 1 7.00
CHEMBL3142703 1 6.80
CHEMBL3142704 1 6.77
CHEMBL3142689 1 6.77
CHEMBL3142687 1 6.64
CHEMBL3142701 1 6.57
CHEMBL3142685 1 6.19
CHEMBL328422 1 6.10
CHEMBL3142686 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3142695 IC50 = 3.6 nM 8.44
CHEMBL320868 IC50 = 3.8 nM 8.42
CHEMBL319340 IC50 = 3.8 nM 8.42
CHEMBL3142693 IC50 = 8.0 nM 8.10
CHEMBL3142705 IC50 = 16.0 nM 7.80
CHEMBL3142683 IC50 = 16.0 nM 7.80
CHEMBL3142682 IC50 = 21.0 nM 7.68
CHEMBL3142903 IC50 = 22.0 nM 7.66
CHEMBL3142694 IC50 = 23.0 nM 7.64
CHEMBL100609 IC50 = 23.0 nM 7.64
CHEMBL3142906 IC50 = 34.0 nM 7.47
CHEMBL3142692 IC50 = 51.0 nM 7.29
CHEMBL3142696 IC50 = 59.0 nM 7.23
CHEMBL3142697 IC50 = 60.0 nM 7.22
CHEMBL3142681 IC50 = 93.0 nM 7.03
CHEMBL3142702 IC50 = 100.0 nM 7.00
CHEMBL3142703 IC50 = 160.0 nM 6.80
CHEMBL3142704 IC50 = 170.0 nM 6.77
CHEMBL3142689 IC50 = 170.0 nM 6.77
CHEMBL3142687 IC50 = 230.0 nM 6.64
CHEMBL3142701 IC50 = 270.0 nM 6.57
CHEMBL3142685 IC50 = 650.0 nM 6.19
CHEMBL328422 IC50 = 800.0 nM 6.10
CHEMBL3142686 IC50 = 12000.0 nM 4.92