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Assay Detail

CHEMBL899634

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Functional
Agonist activity at human GPR109a expressed in human adipocytes assessed as decrease in intracellular cAMP level by HTRF assay
ChEMBL ↗
54
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Hydroxycarboxylic acid receptor 2 (CHEMBL3785) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fluorinated pyrazole acids are agonists of the high affinity niacin receptor GPR109a.
Skinner PJ, Cherrier MC, Webb PJ, Shin YJ, Gharbaoui T, Lindstrom A, Hong V, Tamura SY, Dang HT, Pride CC, Chen R, Richman JG, Connolly DT, Semple G.
Bioorg Med Chem Lett (2007) 17 : 5620 -5623
PubMed 17804224 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 54 6.16 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573 NIACIN 4.0 2 8.06
CHEMBL391574 — — 2 7.61
CHEMBL238004 — — 2 7.38
CHEMBL396864 — — 2 7.24
CHEMBL394498 — — 2 7.10
CHEMBL235009 — — 2 7.10
CHEMBL428730 — — 2 7.07
CHEMBL247098 — — 2 7.00
CHEMBL238002 — — 2 6.96
CHEMBL247921 — — 2 6.96
CHEMBL237788 — — 2 6.74
CHEMBL392859 — — 2 6.57
CHEMBL397055 — — 2 6.12
CHEMBL128679 — — 2 6.11
CHEMBL235228 — — 2 5.82
CHEMBL235231 — — 2 5.82
CHEMBL245491 — — 2 5.65
CHEMBL393062 — — 2 5.60
CHEMBL415261 — — 2 5.53
CHEMBL397056 — — 2 5.46
CHEMBL235010 — — 2 5.36
CHEMBL236728 — — 2 5.23
CHEMBL393064 — — 2 5.11
CHEMBL393063 — — 2 4.77
CHEMBL235230 — — 2 4.74
CHEMBL393065 — — 2 4.73
CHEMBL235229 — — 2 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573 NIACIN EC50 = 8.71 nM 8.06
CHEMBL391574 — EC50 = 24.55 nM 7.61
CHEMBL238004 — EC50 = 41.69 nM 7.38
CHEMBL396864 — EC50 = 57.54 nM 7.24
CHEMBL235009 — EC50 = 79.43 nM 7.10
CHEMBL394498 — EC50 = 79.43 nM 7.10
CHEMBL428730 — EC50 = 85.11 nM 7.07
CHEMBL247098 — EC50 = 100.0 nM 7.00
CHEMBL238002 — EC50 = 109.65 nM 6.96
CHEMBL247921 — EC50 = 109.65 nM 6.96
CHEMBL237788 — EC50 = 181.97 nM 6.74
CHEMBL392859 — EC50 = 269.15 nM 6.57
CHEMBL397055 — EC50 = 758.58 nM 6.12
CHEMBL128679 — EC50 = 776.25 nM 6.11
CHEMBL235228 — EC50 = 1513.56 nM 5.82
CHEMBL235231 — EC50 = 1513.56 nM 5.82
CHEMBL245491 — EC50 = 2238.72 nM 5.65
CHEMBL393062 — EC50 = 2511.89 nM 5.60
CHEMBL415261 — EC50 = 2951.21 nM 5.53
CHEMBL397056 — EC50 = 3467.37 nM 5.46
CHEMBL235010 — EC50 = 4365.16 nM 5.36
CHEMBL236728 — EC50 = 5888.44 nM 5.23
CHEMBL393064 — EC50 = 7762.47 nM 5.11
CHEMBL393063 — EC50 = 16982.44 nM 4.77
CHEMBL235230 — EC50 = 18197.01 nM 4.74
CHEMBL393065 — EC50 = 18620.87 nM 4.73
CHEMBL235229 — EC50 = 40738.03 nM 4.39
CHEMBL236728 — EC50 > 1000.0 nM -
CHEMBL237788 — EC50 > 1000.0 nM -
CHEMBL238002 — EC50 > 1000.0 nM -
CHEMBL247098 — EC50 > 1000.0 nM -
CHEMBL428730 — EC50 > 1000.0 nM -
CHEMBL245491 — EC50 > 1000.0 nM -
CHEMBL247921 — EC50 > 1000.0 nM -
CHEMBL415261 — EC50 > 1000.0 nM -
CHEMBL238004 — EC50 > 1000.0 nM -
CHEMBL396864 — EC50 > 1000.0 nM -
CHEMBL392859 — EC50 > 1000.0 nM -
CHEMBL397056 — EC50 > 1000.0 nM -
CHEMBL397055 — EC50 > 1000.0 nM -
CHEMBL235231 — EC50 > 1000.0 nM -
CHEMBL393065 — EC50 > 1000.0 nM -
CHEMBL235230 — EC50 > 1000.0 nM -
CHEMBL235229 — EC50 > 1000.0 nM -
CHEMBL393064 — EC50 > 1000.0 nM -
CHEMBL235228 — EC50 > 1000.0 nM -
CHEMBL393063 — EC50 > 1000.0 nM -
CHEMBL235010 — EC50 > 1000.0 nM -
CHEMBL393062 — EC50 > 1000.0 nM -
CHEMBL235009 — EC50 > 1000.0 nM -