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Assay Detail

CHEMBL4677903

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

Binding
Displacement of [125I][3-iodo Tyr12,Leu15]gastrin-I from human CCK2R expressed in human A431 cells measured after 1 hr by gamma counter analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-431
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Stabilization Strategies for Linear Minigastrin Analogues: Further Improvements via the Inclusion of Proline into the Peptide Sequence.
Klingler M,Hörmann AA,Rangger C,Desrues L,Castel H,Gandolfo P,von Guggenberg E
J Med Chem (2020) 63 : 14668 -14679
PubMed 33226806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.07 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761587 1 9.40
CHEMBL4759105 1 9.22
CHEMBL4795198 1 9.05
CHEMBL1328 PENTAGASTRIN 4.0 1 9.00
CHEMBL4758706 1 8.89
CHEMBL4795913 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761587 IC50 = 0.4 nM 9.40
CHEMBL4759105 IC50 = 0.6 nM 9.22
CHEMBL4795198 IC50 = 0.9 nM 9.05
CHEMBL1328 PENTAGASTRIN IC50 = 1.0 nM 9.00
CHEMBL4758706 IC50 = 1.3 nM 8.89
CHEMBL4795913 IC50 = 1.4 nM 8.85