Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4124802

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

Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multidose Formulations.
Evers A, Bossart M, Pfeiffer-Marek S, Elvert R, Schreuder H, Kurz M, Stengelin S, Lorenz M, Herling A, Konkar A, Lukasczyk U, Pfenninger A, Lorenz K, Haack T, Kadereit D, Wagner M.
J Med Chem (2018) 61 : 5580 -5593
PubMed 29879354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 8.99 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4127525 1 10.40
CHEMBL4126812 1 10.24
CHEMBL4129347 1 9.99
CHEMBL4128194 1 9.72
CHEMBL4130225 1 9.65
CHEMBL4126027 1 8.94
CHEMBL4128125 1 8.92
CHEMBL4126738 1 8.69
CHEMBL4126953 1 8.69
CHEMBL4130148 1 6.94
CHEMBL4130044 1 6.75
CHEMBL4128112 1 -
CHEMBL4524066 1 -
CHEMBL4128276 1 -
CHEMBL414357 EXENATIDE 4.0 1 -
CHEMBL5314341 GLUCAGON 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4127525 EC50 = 0.0397 nM 10.40
CHEMBL4126812 EC50 = 0.0582 nM 10.24
CHEMBL4129347 EC50 = 0.102 nM 9.99
CHEMBL4128194 EC50 = 0.189 nM 9.72
CHEMBL4130225 EC50 = 0.224 nM 9.65
CHEMBL4126027 EC50 = 1.16 nM 8.94
CHEMBL4128125 EC50 = 1.21 nM 8.92
CHEMBL4126738 EC50 = 2.032 nM 8.69
CHEMBL4126953 EC50 = 2.032 nM 8.69
CHEMBL4130148 EC50 = 114.0 nM 6.94
CHEMBL4130044 EC50 = 177.0 nM 6.75
CHEMBL4128112 EC50 > 1.0 10'8pM -
CHEMBL4524066 EC50 > 1.0 10'8pM -
CHEMBL4128276 EC50 > 1.0 10'8pM -
CHEMBL414357 EXENATIDE EC50 = 2.0 10'5pM -
CHEMBL5314341 GLUCAGON EC50 > 1.0 10'8pM -