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Assay Detail

CHEMBL1680944

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Functional
Agonist activity at human recombinant GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL ↗
48
Total Activities
48
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

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

Publication

Discovery of a potent nicotinic Acid receptor agonist for the treatment of dyslipidemia.
Qin J, Rao A, Chen X, Zhu X, Liu Z, Huang X, Degrado S, Huang Y, Xiao D, Aslanian R, Cheewatrakoolpong B, Zhang H, Greenfeder S, Farley C, Cook J, Kurowski S, Li Q, van Heek M, Chintala M, Wang G, Hsieh Y, Li F, Palani A.
ACS Med Chem Lett (2011) 2 : 171 -176
PubMed 24900295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 48 6.21 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672639 — — 1 7.31
CHEMBL1671877 — — 1 7.23
CHEMBL573 NIACIN 4.0 1 7.00
CHEMBL1672732 — — 1 6.97
CHEMBL1672751 — — 1 6.89
CHEMBL1672738 — — 1 6.89
CHEMBL1672750 — — 1 6.61
CHEMBL1672753 — — 1 6.56
CHEMBL1672645 — — 1 6.55
CHEMBL1672752 — — 1 6.51
CHEMBL1672640 — — 1 6.49
CHEMBL1672744 — — 1 6.47
CHEMBL1672743 — — 1 6.45
CHEMBL1672737 — — 1 6.42
CHEMBL1672733 — — 1 6.35
CHEMBL1672755 — — 1 6.33
CHEMBL1672736 — — 1 6.32
CHEMBL1672741 — — 1 6.23
CHEMBL1672641 — — 1 6.10
CHEMBL1672735 — — 1 6.09
CHEMBL1672642 — — 1 5.97
CHEMBL1672767 — — 1 5.96
CHEMBL1672742 — — 1 5.90
CHEMBL1672637 — — 1 5.85
CHEMBL1672745 — — 1 5.57
CHEMBL1672638 — — 1 5.51
CHEMBL1672643 — — 1 5.51
CHEMBL1672768 — — 1 5.47
CHEMBL1672754 — — 1 5.38
CHEMBL1672749 — — 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672639 — EC50 = 49.0 nM 7.31
CHEMBL1671877 — EC50 = 59.0 nM 7.23
CHEMBL573 NIACIN EC50 = 100.0 nM 7.00
CHEMBL1672732 — EC50 = 108.0 nM 6.97
CHEMBL1672751 — EC50 = 128.0 nM 6.89
CHEMBL1672738 — EC50 = 130.0 nM 6.89
CHEMBL1672750 — EC50 = 245.0 nM 6.61
CHEMBL1672753 — EC50 = 275.0 nM 6.56
CHEMBL1672645 — EC50 = 281.0 nM 6.55
CHEMBL1672752 — EC50 = 308.0 nM 6.51
CHEMBL1672640 — EC50 = 327.0 nM 6.49
CHEMBL1672744 — EC50 = 335.0 nM 6.47
CHEMBL1672743 — EC50 = 353.0 nM 6.45
CHEMBL1672737 — EC50 = 379.0 nM 6.42
CHEMBL1672733 — EC50 = 451.0 nM 6.35
CHEMBL1672755 — EC50 = 470.0 nM 6.33
CHEMBL1672736 — EC50 = 479.0 nM 6.32
CHEMBL1672741 — EC50 = 591.0 nM 6.23
CHEMBL1672641 — EC50 = 787.0 nM 6.10
CHEMBL1672735 — EC50 = 821.0 nM 6.09
CHEMBL1672642 — EC50 = 1076.0 nM 5.97
CHEMBL1672767 — EC50 = 1110.0 nM 5.96
CHEMBL1672742 — EC50 = 1261.0 nM 5.90
CHEMBL1672637 — EC50 = 1402.0 nM 5.85
CHEMBL1672745 — EC50 = 2705.0 nM 5.57
CHEMBL1672643 — EC50 = 3119.0 nM 5.51
CHEMBL1672638 — EC50 = 3108.0 nM 5.51
CHEMBL1672768 — EC50 = 3393.0 nM 5.47
CHEMBL1672754 — EC50 = 4152.0 nM 5.38
CHEMBL1672749 — EC50 = 4436.0 nM 5.35
CHEMBL1672746 — EC50 = 6065.0 nM 5.22
CHEMBL1672748 — EC50 = 6581.0 nM 5.18
CHEMBL1672756 — EC50 > 10000.0 nM -
CHEMBL1672757 — EC50 > 10000.0 nM -
CHEMBL1672758 — EC50 > 10000.0 nM -
CHEMBL1672759 — EC50 > 10000.0 nM -
CHEMBL1672760 — EC50 > 10000.0 nM -
CHEMBL1672761 — EC50 > 10000.0 nM -
CHEMBL1672762 — EC50 > 10000.0 nM -
CHEMBL1672763 — EC50 > 10000.0 nM -
CHEMBL1672764 — EC50 > 10000.0 nM -
CHEMBL1672765 — EC50 > 10000.0 nM -
CHEMBL1672766 — EC50 > 10000.0 nM -
CHEMBL1672747 — EC50 > 10000.0 nM -
CHEMBL1672734 — EC50 > 10000.0 nM -
CHEMBL1672739 — EC50 > 10000.0 nM -
CHEMBL1672644 — EC50 > 10000.0 nM -
CHEMBL1672740 — EC50 > 10000.0 nM -