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Assay Detail

CHEMBL3865595

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Binding
Agonist activity at human GPR40 expressed in HEK293 cells measured after 18 to 20 hrs by beta-gal based luciferase reporter gene assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Free fatty acid receptor 1 (CHEMBL4422)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist.
Agarwal S, Sasane S, Deshmukh P, Rami B, Bandyopadhyay D, Giri P, Giri S, Jain M, Desai RC.
ACS Med Chem Lett (2016) 7 : 1134 -1138
PubMed 27994752 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 8.16 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3922381 1 9.10
CHEMBL3904378 1 8.85
CHEMBL3896509 1 8.72
CHEMBL1829174 FASIGLIFAM 3.0 1 8.72
CHEMBL3966739 1 8.72
CHEMBL3923431 1 8.70
CHEMBL3889768 1 8.68
CHEMBL1829173 1 8.66
CHEMBL3924534 1 8.36
CHEMBL3951157 1 8.34
CHEMBL3918387 1 8.15
CHEMBL3914686 1 8.11
CHEMBL3914418 1 8.10
CHEMBL3975239 1 8.07
CHEMBL3913383 1 8.07
CHEMBL3893141 1 8.00
CHEMBL3957744 1 7.92
CHEMBL3895442 1 7.79
CHEMBL3933446 1 7.78
CHEMBL3921143 1 7.53
CHEMBL3894356 1 7.42
CHEMBL3931296 1 6.93
CHEMBL3905435 1 6.85
CHEMBL3964251 1 -
CHEMBL3902108 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3922381 EC50 = 0.8 nM 9.10
CHEMBL3904378 EC50 = 1.4 nM 8.85
CHEMBL3896509 EC50 = 1.9 nM 8.72
CHEMBL1829174 FASIGLIFAM EC50 = 1.9 nM 8.72
CHEMBL3966739 EC50 = 1.9 nM 8.72
CHEMBL3923431 EC50 = 2.0 nM 8.70
CHEMBL3889768 EC50 = 2.1 nM 8.68
CHEMBL1829173 EC50 = 2.2 nM 8.66
CHEMBL3924534 EC50 = 4.4 nM 8.36
CHEMBL3951157 EC50 = 4.6 nM 8.34
CHEMBL3918387 EC50 = 7.0 nM 8.15
CHEMBL3914686 EC50 = 7.7 nM 8.11
CHEMBL3914418 EC50 = 7.9 nM 8.10
CHEMBL3975239 EC50 = 8.6 nM 8.07
CHEMBL3913383 EC50 = 8.6 nM 8.07
CHEMBL3893141 EC50 = 10.0 nM 8.00
CHEMBL3957744 EC50 = 12.0 nM 7.92
CHEMBL3895442 EC50 = 16.1 nM 7.79
CHEMBL3933446 EC50 = 16.7 nM 7.78
CHEMBL3921143 EC50 = 29.6 nM 7.53
CHEMBL3894356 EC50 = 38.0 nM 7.42
CHEMBL3931296 EC50 = 118.3 nM 6.93
CHEMBL3905435 EC50 = 140.0 nM 6.85
CHEMBL3964251 EC50 > 1000.0 nM -
CHEMBL3902108 EC50 - -