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Assay Detail

CHEMBL4677904

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Functional
Agonist activity at human CCK2R expressed in human A431 cells assessed as intracellular calcium mobilization measured after 24 hrs by Fluo-4AM dye based fluorimetry analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 4 8.06 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1328 PENTAGASTRIN 4.0 1 8.55
CHEMBL4758706 1 7.91
CHEMBL4795913 1 7.91
CHEMBL4759105 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1328 PENTAGASTRIN EC50 = 2.8 nM 8.55
CHEMBL4758706 EC50 = 12.38 nM 7.91
CHEMBL4795913 EC50 = 12.34 nM 7.91
CHEMBL4759105 EC50 = 14.23 nM 7.85