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Assay Detail

CHEMBL1833690

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Functional
Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry
ChEMBL ↗
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 1321-N1
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 a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.
Christiansen E, Urban C, Grundmann M, Due-Hansen ME, Hagesaether E, Schmidt J, Pardo L, Ullrich S, Kostenis E, Kassack M, Ulven T.
J Med Chem (2011) 54 : 6691 -6703
PubMed 21854074 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 6.41 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1688473 — — 1 8.22
CHEMBL1829174 FASIGLIFAM 3.0 1 7.85
CHEMBL1773261 — — 1 7.73
CHEMBL1829170 — — 1 7.39
CHEMBL1829172 — — 1 7.37
CHEMBL1829171 — — 1 7.36
CHEMBL449588 — — 1 7.34
CHEMBL207881 GW9508 — 1 7.32
CHEMBL1829156 — — 1 7.12
CHEMBL1829169 — — 1 7.10
CHEMBL604126 — — 1 7.06
CHEMBL1829173 — — 1 7.00
CHEMBL1829165 — — 1 6.92
CHEMBL1829166 — — 1 6.87
CHEMBL1829164 — — 1 6.75
CHEMBL1829162 — — 1 6.73
CHEMBL488384 — — 1 6.70
CHEMBL1829155 — — 1 6.60
CHEMBL1829159 — — 1 6.53
CHEMBL389699 — — 1 6.52
CHEMBL1829167 — — 1 6.50
CHEMBL1829161 — — 1 6.32
CHEMBL1829158 — — 1 6.29
CHEMBL1829160 — — 1 6.28
CHEMBL1829148 — — 1 6.22
CHEMBL1829150 — — 1 6.18
CHEMBL1829149 — — 1 6.15
CHEMBL1829168 — — 1 6.10
CHEMBL1829163 — — 1 5.97
CHEMBL1829157 — — 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1688473 — EC50 = 6.026 nM 8.22
CHEMBL1829174 FASIGLIFAM EC50 = 14.13 nM 7.85
CHEMBL1773261 — EC50 = 18.62 nM 7.73
CHEMBL1829170 — EC50 = 40.74 nM 7.39
CHEMBL1829172 — EC50 = 42.66 nM 7.37
CHEMBL1829171 — EC50 = 43.65 nM 7.36
CHEMBL449588 — EC50 = 45.71 nM 7.34
CHEMBL207881 GW9508 EC50 = 47.86 nM 7.32
CHEMBL1829156 — EC50 = 75.86 nM 7.12
CHEMBL1829169 — EC50 = 79.43 nM 7.10
CHEMBL604126 — EC50 = 87.1 nM 7.06
CHEMBL1829173 — EC50 = 100.0 nM 7.00
CHEMBL1829165 — EC50 = 120.23 nM 6.92
CHEMBL1829166 — EC50 = 134.9 nM 6.87
CHEMBL1829164 — EC50 = 177.83 nM 6.75
CHEMBL1829162 — EC50 = 186.21 nM 6.73
CHEMBL488384 — EC50 = 199.53 nM 6.70
CHEMBL1829155 — EC50 = 251.19 nM 6.60
CHEMBL1829159 — EC50 = 295.12 nM 6.53
CHEMBL389699 — EC50 = 302.0 nM 6.52
CHEMBL1829167 — EC50 = 316.23 nM 6.50
CHEMBL1829161 — EC50 = 478.63 nM 6.32
CHEMBL1829158 — EC50 = 512.86 nM 6.29
CHEMBL1829160 — EC50 = 524.81 nM 6.28
CHEMBL1829148 — EC50 = 602.56 nM 6.22
CHEMBL1829150 — EC50 = 660.69 nM 6.18
CHEMBL1829149 — EC50 = 707.95 nM 6.15
CHEMBL1829168 — EC50 = 794.33 nM 6.10
CHEMBL1829163 — EC50 = 1071.52 nM 5.97
CHEMBL1829157 — EC50 = 1122.02 nM 5.95
CHEMBL1829153 — EC50 = 2754.23 nM 5.56
CHEMBL1829154 — EC50 = 3890.45 nM 5.41
CHEMBL1829145 — EC50 = 4073.8 nM 5.39
CHEMBL1829142 — EC50 = 4265.8 nM 5.37
CHEMBL1829144 — EC50 = 6025.6 nM 5.22
CHEMBL1829146 — EC50 = 6165.95 nM 5.21
CHEMBL1829151 — EC50 = 9120.11 nM 5.04
CHEMBL1829152 — EC50 = 9549.93 nM 5.02
CHEMBL1829147 — EC50 = 10964.78 nM 4.96
CHEMBL1829143 — EC50 = 13182.57 nM 4.88