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Assay Detail

CHEMBL995931

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

Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Gastric inhibitory polypeptide receptor (CHEMBL4383)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties.
Madsen P, Kodra JT, Behrens C, Nishimura E, Jeppesen CB, Pridal L, Andersen B, Knudsen LB, Valcarce-Aspegren C, Guldbrandt M, Christensen IT, Jørgensen AS, Ynddal L, Brand CL, Bagger MA, Lau J.
J Med Chem (2009) 52 : 2989 -3000
PubMed 19385613 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.37 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491920 1 6.68
CHEMBL455323 1 6.54
CHEMBL523847 1 6.53
CHEMBL448561 1 6.50
CHEMBL492813 1 6.41
CHEMBL451288 1 6.41
CHEMBL471580 1 6.39
CHEMBL519776 1 6.34
CHEMBL501628 1 6.32
CHEMBL492605 1 6.29
CHEMBL446821 1 6.11
CHEMBL470729 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491920 IC50 = 211.0 nM 6.68
CHEMBL455323 IC50 = 290.0 nM 6.54
CHEMBL523847 IC50 = 293.0 nM 6.53
CHEMBL448561 IC50 = 320.0 nM 6.50
CHEMBL492813 IC50 = 390.0 nM 6.41
CHEMBL451288 IC50 = 390.0 nM 6.41
CHEMBL471580 IC50 = 410.0 nM 6.39
CHEMBL519776 IC50 = 460.0 nM 6.34
CHEMBL501628 IC50 = 480.0 nM 6.32
CHEMBL492605 IC50 = 510.0 nM 6.29
CHEMBL446821 IC50 = 770.0 nM 6.11
CHEMBL470729 IC50 = 1100.0 nM 5.96