Protein Information

General Information of the Protein

Protein ID	PT04975
Protein Name	G-protein coupled bile acid receptor 1
Secondarily Protein Name	Membrane-type receptor for bile acids
Gene Name	GPBAR1
Secondarily Gene Name	Tgr5
Sequence	MMTPNSTELSAIPMGVLGLSLALASLIVIANLLLALGIALDRHLRSPPAGCFFLSLLLAGLLTGLALPMLPGLWSRNHQGYWSCLLLHLTPNFCFLSLLANLLLVHGERYMAVLQPLRPHGSVRLALFLTWVSSLFFASLPALGWNHWSPDANCSSQAVFPAPYLYLEVYGLLLPAVGATALLSVRVLATAHRQLCEIRRLERAVCRDVPSTLARALTWRQARAQAGATLLFLLCWGPYVATLLLSVLAYERRPPLGPGTLLSLISLGSTSAAAVPVAMGLGDQRYTAPWRTAAQRCLRVLRGRAKRDNPGPSTAYHTSSQCSIDLDLN Show/Hide
Organism	Mus musculus, Mouse
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Small molecule receptor (family A GPCR) > Lipid-like ligand receptor (family A GPCR) > Steroid-like ligand receptor
Function	Receptor for bile acid. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of macrophage functions by bile acids (By similarity). Involved in bile acid promoted GLP1R secretion. Show/Hide
Uniprot ID	Q80SS6
Ensembl ID	ENSG00000179921
Subcellular Location	Cell membrane

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000011 , CHO

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0851544 Compound Info	(R,E)-1-(4-(3-(hydroxyimino)-3-(2-methylpyridin-4-yl)-1-o-tolylpropyl)phenyl)piperidine-4-carboxylic acid Show/Hide	C28H31N3O3	1
1	EC50 = 28 nM Bioactivity Info	TI LI LO TS
CP0857946 Compound Info	4'-(3-(hydroxyimino)-3-(2-methylpyridin-4-yl)-1-o-tolylpropyl)biphenyl-4-carboxylic acid Show/Hide	C29H26N2O3	1
1	EC50 = 93 nM Bioactivity Info	TI LI LO TS
CP0857958 Compound Info	(S,E)-1-(4-(3-(hydroxyimino)-3-(2-methylpyridin-4-yl)-1-o-tolylpropyl)phenyl)piperidine-4-carboxylic acid Show/Hide	C28H31N3O3	1
1	EC50 = 130 nM Bioactivity Info	TI LI LO TS
CP0857947 Compound Info	(R,E)-4'-(3-(hydroxyimino)-3-(2-methylpyridin-4-yl)-1-o-tolylpropyl)biphenyl-4-carboxylic acid Show/Hide	C29H26N2O3	1
1	EC50 = 140 nM Bioactivity Info	TI LI LO TS
CP0851546 Compound Info	(S,E)-4'-(3-(hydroxyimino)-3-(2-methylpyridin-4-yl)-1-o-tolylpropyl)biphenyl-4-carboxylic acid Show/Hide	C29H26N2O3	1
1	EC50 = 190 nM Bioactivity Info	TI LI LO TS
CP0857927 Compound Info	3-(4-bromophenyl)-1-(pyridin-4-yl)-3-o-tolylpropan-1-one oxime Show/Hide	C21H19BrN2O	1
1	EC50 = 310 nM Bioactivity Info	TI LI LO TS
CP0913115 Compound Info	(R,E)-4'-(3-(hydroxyimino)-3-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1-o-tolylpropyl)biphenyl-4-carboxylic acid Show/Hide	C29H26N2O4	1
1	EC50 = 450 nM Bioactivity Info	TI LI LO TS
CP0906563 Compound Info	(S,E)-4'-(3-(hydroxyimino)-3-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1-o-tolylpropyl)biphenyl-4-carboxylic acid Show/Hide	C29H26N2O4	1
1	EC50 = 620 nM Bioactivity Info	TI LI LO TS
CP0913130 Compound Info	3-(4-(dimethylamino)phenyl)-1-(pyridin-4-yl)-3-o-tolylpropan-1-one oxime Show/Hide	C23H25N3O	1
1	EC50 = 700 nM Bioactivity Info	TI LI LO TS
CP0909363 Compound Info	3-(4-bromophenyl)-1-(2-methylpyridin-4-yl)-3-o-tolylpropan-1-one oxime Show/Hide	C22H21BrN2O	1
1	EC50 = 740 nM Bioactivity Info	TI LI LO TS
CP0864598 Compound Info	4'-(3-(hydroxyimino)-3-(2-methylpyridin-4-yl)-1-o-tolylpropyl)biphenyl-3-carboxylic acid Show/Hide	C29H26N2O3	1
1	EC50 = 860 nM Bioactivity Info	TI LI LO TS
CP0909410 Compound Info	3-(4-(dimethylamino)phenyl)-1-(pyridin-4-yl)-3-p-tolylpropan-1-one oxime Show/Hide	C23H25N3O	1
1	EC50 = 1100 nM Bioactivity Info	TI LI LO TS
CP0873888 Compound Info	(R,E)-5-(1-(hydroxyimino)-3-(4-(methylsulfonyl)phenyl)-3-o-tolylpropyl)-1-methylpyridin-2(1H)-one Show/Hide	C23H24N2O4S	1
1	EC50 = 1300 nM Bioactivity Info	TI LI LO TS
CP0906564 Compound Info	5-(3-(4-bromophenyl)-1-(hydroxyimino)-3-o-tolylpropyl)-1-methylpyridin-2(1H)-one Show/Hide	C22H21BrN2O2	1
1	EC50 = 1420 nM Bioactivity Info	TI LI LO TS
CP0857959 Compound Info	3-(4-(dimethylamino)phenyl)-1-(pyridin-4-yl)-3-m-tolylpropan-1-one oxime Show/Hide	C23H25N3O	1
1	EC50 = 1500 nM Bioactivity Info	TI LI LO TS
CP0857929 Compound Info	3-(4-(dimethylamino)phenyl)-3-(pyridin-2-yl)-1-(pyridin-4-yl)propan-1-one oxime Show/Hide	C21H22N4O	1
1	EC50 = 1600 nM Bioactivity Info	TI LI LO TS
CP0851545 Compound Info	(E)-3-(4-(dimethylamino)phenyl)-3-phenyl-1-(pyridin-4-yl)propan-1-one oxime Show/Hide	C22H23N3O	1
1	EC50 = 2000 nM Bioactivity Info	TI LI LO TS
CP0906562 Compound Info	(S,E)-5-(1-(hydroxyimino)-3-(4-(methylsulfonyl)phenyl)-3-o-tolylpropyl)-1-methylpyridin-2(1H)-one Show/Hide	C23H24N2O4S	1
1	EC50 = 3000 nM Bioactivity Info	TI LI LO TS
CP0913131 Compound Info	4-(3-(hydroxyimino)-3-(2-methylpyridin-4-yl)-1-o-tolylpropyl)benzoic acid Show/Hide	C23H22N2O3	1
1	EC50 = 3700 nM Bioactivity Info	TI LI LO TS
CP0146999 Compound Info	2-(ethylamino)-6-[3-(4-propan-2-ylphenyl)propanoyl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidine-4-carboxamide Show/Hide	C22H29N5O2	1
1	EC50 = 5620 nM Bioactivity Info	TI LI LO TS
CP0857960 Compound Info	2-(4-(3-(hydroxyimino)-3-(2-methylpyridin-4-yl)-1-o-tolylpropyl)phenyl)acetic acid Show/Hide	C24H24N2O3	1
1	EC50 = 6100 nM Bioactivity Info	TI LI LO TS