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Assay Detail

CHEMBL661233

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

Binding
Compound was tested for its inhibitory activity in pancreatic cholecystokinin type A receptor in guinea pig
5
Total Activities
5
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

trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline.
Holladay MW, Lin CW, May CS, Garvey DS, Witte DG, Miller TR, Wolfram CA, Nadzan AM.
J Med Chem (1991) 34 : 455 -457
PubMed 1992147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.48 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64605 1 5.75
CHEMBL2370879 1 5.68
CHEMBL3143186 1 5.57
CHEMBL169054 1 5.40
CHEMBL333299 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64605 IC50 = 1800.0 nM 5.75
CHEMBL2370879 IC50 = 2100.0 nM 5.68
CHEMBL3143186 IC50 = 2700.0 nM 5.57
CHEMBL169054 IC50 = 4000.0 nM 5.40
CHEMBL333299 IC50 = 10300.0 nM 4.99