A-431
|
EC50 |
|
Activation of GPR109A in human A431 cells assessed as suppression of forskolin-induced cAMP production after 30 mins
Activation of GPR109A in human A431 cells assessed as suppression of forskolin-induced cAMP production after 30 mins
|
[PMID: 26784936]
|
Adipocyte
|
IC50 |
|
Inhibition of lipolysis in IBMX-stimulated human adipocytes assessed as glycerol release after 5 hrs
Inhibition of lipolysis in IBMX-stimulated human adipocytes assessed as glycerol release after 5 hrs
|
[PMID: 19309152]
|
Adipocyte
|
EC50 |
|
Inhibition of isoproterenol-induced lipolysis in human subcutaneous adipocytes after 5 hrs
Inhibition of isoproterenol-induced lipolysis in human subcutaneous adipocytes after 5 hrs
|
[PMID: 17452318]
|
CCRF-CEM
|
IC50 |
> 500 μM
Compound: Niacin
|
Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by coulter counter method
Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by coulter counter method
|
[PMID: 28238612]
|
CHO
|
EC50 |
0.027 μM
Compound: Niacin
|
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
Agonist activity at GPR109a expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production by HTRF assay
|
[PMID: 20363624]
|
CHO
|
EC50 |
1 μM
Compound: nicotinic acid
|
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
[PMID: 18752940]
|
CHO
|
IC50 |
|
Agonist activity at human niacin receptor expressed in CHO cells by GTPgammaS binding assay
Agonist activity at human niacin receptor expressed in CHO cells by GTPgammaS binding assay
|
[PMID: 18477506]
|
CHO
|
EC50 |
51 nM
Compound: niacin, Niaspan
|
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
Agonist activity at human GPR109a expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP production by HTRF assay
|
[PMID: 22435740]
|
CHO-K1
|
EC50 |
|
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTPgammaS binding assay
|
[PMID: 19309152]
|
CHO-K1
|
EC50 |
|
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
Agonist activity at human GPR109A expressed in CHOK1 cells by [35S]GTP-gamma-S binding assay
|
[PMID: 17994679]
|
CHO-K1
|
EC50 |
1.4 μM
Compound: nicotinic acid
|
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
|
[PMID: 18760600]
|
CHO-K1
|
EC50 |
47 nM
Compound: Nicotinic acid
|
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
Agonist activity at HCA2 receptor (unknown origin) expressed in CHOK1 cells assessed as ERK1/2 phosphorylation by ELISA
|
[PMID: 25737085]
|
CHO-K1
|
EC50 |
|
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at cloned human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
|
[PMID: 20184326]
|
CHO-K1
|
EC50 |
|
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
Activation of GPR109A receptor in CHOK1 cells assessed as ERK1/2 MAP kinase activation by ELISA
|
[PMID: 17452318]
|
CHO-K1
|
IC50 |
|
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
|
[PMID: 17452318]
|
COS-7
|
EC50 |
|
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
Agonist activity at human recombinant GPR109a transfected in african green monkey COS-7 cells after 20 mins by [35S]GTPgammaS binding assay
|
[PMID: 24900524]
|
HEK293
|
IC50 |
> 500 μM
Compound: niacin
|
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
|
[PMID: 23241029]
|
HEK-293T
|
IC50 |
249 nM
Compound: Nicotinic acid
|
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
|
[PMID: 25737085]
|
HEK-293T
|
EC50 |
|
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
Agonist activity at GPR109A receptor (unknown origin) expressed in HEK293T cell membranes after 30 mins by [35S]GTPgammaS binding based microbeta scintillation counting analysis
|
[PMID: 32199732]
|
HL-60
|
CC50 |
> 200 μM
Compound: Niacin
|
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
|
[PMID: 28238612]
|
HSC-2
|
CC50 |
> 200 μM
Compound: Niacin
|
Cytotoxicity against human HSC2 cells after 48 hrs by MTT assay
Cytotoxicity against human HSC2 cells after 48 hrs by MTT assay
|
[PMID: 28238612]
|
HSC-3
|
CC50 |
> 200 μM
Compound: Niacin
|
Cytotoxicity against human HSC3 cells after 48 hrs by MTT assay
Cytotoxicity against human HSC3 cells after 48 hrs by MTT assay
|
[PMID: 28238612]
|
HSC-4
|
CC50 |
> 200 μM
Compound: Niacin
|
Cytotoxicity against human HSC4 cells after 48 hrs by MTT assay
Cytotoxicity against human HSC4 cells after 48 hrs by MTT assay
|
[PMID: 28238612]
|
L1210
|
IC50 |
> 500 μM
Compound: Niacin
|
Cytotoxicity against mouse L1210 cells assessed as growth inhibition after 48 hrs by coulter counter method
Cytotoxicity against mouse L1210 cells assessed as growth inhibition after 48 hrs by coulter counter method
|
[PMID: 28238612]
|