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Assay Detail

CHEMBL2383047

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Functional
Agonist activity at human GPR40 transfected in CHO cells by calcium flux assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel orally bioavailable GPR40 agonists.
Lu H, Fei H, Yang F, Zheng S, Hu Q, Zhang L, Yuan J, Feng J, Sun P, Dong Q.
Bioorg Med Chem Lett (2013) 23 : 2920 -2924
PubMed 23582779 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 41 7.20 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381289 1 7.95
CHEMBL2381282 1 7.87
CHEMBL2381287 1 7.80
CHEMBL2381308 1 7.72
CHEMBL2381306 1 7.52
CHEMBL2381290 1 7.52
CHEMBL2381285 1 7.47
CHEMBL2381312 1 7.45
CHEMBL2381291 1 7.44
CHEMBL2381307 1 7.41
CHEMBL2381313 1 7.41
CHEMBL2047159 1 7.38
CHEMBL2381295 1 7.33
CHEMBL2381305 1 7.28
CHEMBL2381281 1 7.26
CHEMBL2381293 1 7.25
CHEMBL2381310 1 7.25
CHEMBL2381302 1 7.25
CHEMBL2381314 1 7.21
CHEMBL2380322 1 7.20
CHEMBL2381311 1 7.18
CHEMBL2381309 1 7.18
CHEMBL2381296 1 7.17
CHEMBL2381280 1 7.13
CHEMBL2381318 1 7.13
CHEMBL2381317 1 7.13
CHEMBL2381297 1 7.08
CHEMBL2381315 1 7.06
CHEMBL2381299 1 7.02
CHEMBL2381292 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381289 EC50 = 11.3 nM 7.95
CHEMBL2381282 EC50 = 13.5 nM 7.87
CHEMBL2381287 EC50 = 16.0 nM 7.80
CHEMBL2381308 EC50 = 19.1 nM 7.72
CHEMBL2381306 EC50 = 30.1 nM 7.52
CHEMBL2381290 EC50 = 30.4 nM 7.52
CHEMBL2381285 EC50 = 34.2 nM 7.47
CHEMBL2381312 EC50 = 35.9 nM 7.45
CHEMBL2381291 EC50 = 36.4 nM 7.44
CHEMBL2381307 EC50 = 39.3 nM 7.41
CHEMBL2381313 EC50 = 38.7 nM 7.41
CHEMBL2047159 EC50 = 41.8 nM 7.38
CHEMBL2381295 EC50 = 46.5 nM 7.33
CHEMBL2381305 EC50 = 52.9 nM 7.28
CHEMBL2381281 EC50 = 54.7 nM 7.26
CHEMBL2381293 EC50 = 55.9 nM 7.25
CHEMBL2381302 EC50 = 56.2 nM 7.25
CHEMBL2381310 EC50 = 56.7 nM 7.25
CHEMBL2381314 EC50 = 61.6 nM 7.21
CHEMBL2380322 EC50 = 63.7 nM 7.20
CHEMBL2381311 EC50 = 65.4 nM 7.18
CHEMBL2381309 EC50 = 66.7 nM 7.18
CHEMBL2381296 EC50 = 67.5 nM 7.17
CHEMBL2381280 EC50 = 74.5 nM 7.13
CHEMBL2381318 EC50 = 73.2 nM 7.13
CHEMBL2381317 EC50 = 74.7 nM 7.13
CHEMBL2381297 EC50 = 82.4 nM 7.08
CHEMBL2381315 EC50 = 88.0 nM 7.06
CHEMBL2381299 EC50 = 94.8 nM 7.02
CHEMBL2381292 EC50 = 105.1 nM 6.98
CHEMBL2381283 EC50 = 111.1 nM 6.95
CHEMBL2381298 EC50 = 120.7 nM 6.92
CHEMBL2381301 EC50 = 122.6 nM 6.91
CHEMBL2381304 EC50 = 125.0 nM 6.90
CHEMBL2381316 EC50 = 132.0 nM 6.88
CHEMBL2381300 EC50 = 145.2 nM 6.84
CHEMBL2381288 EC50 = 190.5 nM 6.72
CHEMBL2381303 EC50 = 205.1 nM 6.69
CHEMBL2381286 EC50 = 219.8 nM 6.66
CHEMBL2381294 EC50 = 282.0 nM 6.55
CHEMBL2381284 EC50 > 10000.0 nM -