Protein Information

General Information of the Protein

Protein ID	PT03505
Protein Name	Ileal sodium/bile acid cotransporter
Secondarily Protein Name	Apical sodium-dependent bile acid transporter Ileal Na(+)/bile acid cotransporter Ileal sodium-dependent bile acid transporter Na(+)-dependent ileal bile acid transporter Sodium/taurocholate cotransporting polypeptide ileal Solute carrier family 10 member 2
Gene Name	SLC10A2
Secondarily Gene Name	ASBT ISBT NTCP2
Sequence	MNDPNSCVDNATVCSGASCVVPESNFNNILSVVLSTVLTILLALVMFSMGCNVEIKKFLGHIKRPWGICVGFLCQFGIMPLTGFILSVAFDILPLQAVVVLIIGCCPGGTASNILAYWVDGDMDLSVSMTTCSTLLALGMMPLCLLIYTKMWVDSGSIVIPYDNIGTSLVSLVVPVSIGMFVNHKWPQKAKIILKIGSIAGAILIVLIAVVGGILYQSAWIIAPKLWIIGTIFPVAGYSLGFLLARIAGLPWYRCRTVAFETGMQNTQLCSTIVQLSFTPEELNVVFTFPLIYSIFQLAFAAIFLGFYVAYKKCHGKNKAEIPESKENGTEPESSFYKANGGFQPDEK Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Transporter > Electrochemical transporter > SLC superfamily of solute carriers > SLC10 family of sodium-bile acid co-transporters
Function	Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine (PubMed:7592981, PubMed:9458785, PubMed:9856990). Transports various bile acids, unconjugated or conjugated, such as cholate and taurocholate (PubMed:7592981, PubMed:9458785, PubMed:9856990). Also responsible for bile acid transport in the renal proximal tubules, a salvage mechanism that helps conserve bile acids (Probable). Works collaboratively with the Na(+)-taurocholate cotransporting polypeptide (NTCP), the organic solute transporter (OST), and the bile salt export pump (BSEP), to ensure efficacious biological recycling of bile acids during enterohepatic circulation (PubMed:33222321). Show/Hide
Uniprot ID	Primary ID: Q12908 Secondarily ID: A1L4F4 Q13839 Show/Hide
Ensembl ID	ENSG00000125255
HGNC ID	HGNC:10906
Subcellular Location	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: CL000051 , BHK-21

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0897873 Compound Info	Trifluoro-acetate{4-[3-((8R,9R)-7,7-dibutyl-2-dimethylamino-8-hydroxy-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenylcarbamoyl]-butyl}-triethyl-ammonium Show/Hide	C38H59F3N4O6S	1
1	IC50 = 1.6 nM Bioactivity Info	TI LI LO TS
CP0929261 Compound Info	[2-(2-{2-[4-((8R,9R)-7,7-Dibutyl-2-dimethylamino-8-hydroxy-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenoxy]-ethoxy}-ethoxy)-ethyl]-triethyl-ammonium iodide Show/Hide	C37H62IN3O6S	1
1	IC50 = 3 nM Bioactivity Info	TI LI LO TS
CP0464444 Compound Info	(8R,9R)-9-(3-Amino-phenyl)-7,7-dibutyl-2-dimethylamino-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C25H37N3O3S	1
1	IC50 = 6 nM Bioactivity Info	TI LI LO TS
CP0532379 Compound Info	(8R,9R)-7,7-Dibutyl-2-dimethylamino-9-(4-hydroxy-phenyl)-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C25H36N2O4S	1
1	IC50 = 8 nM Bioactivity Info	TI LI LO TS
CP0520306 Compound Info	5-Bromo-pentanoic acid [3-((8R,9R)-7,7-dibutyl-2-dimethylamino-8-hydroxy-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenyl]-amide Show/Hide	C30H44BrN3O4S	1
1	IC50 = 22 nM Bioactivity Info	TI LI LO TS
CP0392222 Compound Info	(8R,9R)-7,7-Dibutyl-2-dimethylamino-9-(4-methoxy-phenyl)-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C26H38N2O4S	1
1	IC50 = 26 nM Bioactivity Info	TI LI LO TS
CP0463547 Compound Info	(8R,9R)-7,7-Dibutyl-2-dimethylamino-5,5-dioxo-9-phenyl-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C25H36N2O3S	1
1	IC50 = 35 nM Bioactivity Info	TI LI LO TS
CP0528824 Compound Info	(8R,9R)-7,7-Dibutyl-2-dimethylamino-9-(3-nitro-phenyl)-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C25H35N3O5S	1
1	IC50 = 44 nM Bioactivity Info	TI LI LO TS
CP0407416 Compound Info	(7R,9R)-7-Butyl-7-ethyl-2,3-dimethoxy-9-phenyl-6,7,8,9-tetrahydro-5-thia-8-aza-benzocycloheptene 5,5-dioxide Show/Hide	C23H31NO4S	1
1	IC50 = 48 nM Bioactivity Info	TI LI LO TS
CP0893932 Compound Info	{4-[3-((8R,9R)-7,7-Dibutyl-2-dimethylamino-8-hydroxy-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenylcarbamoyl]-butyl}-triethyl-ammonium bromide Show/Hide	C37H61BrN4O4S	1
1	IC50 = 83 nM Bioactivity Info	TI LI LO TS
CP0880858 Compound Info	[2-(2-{2-[4-((8R,9R)-7,7-Dibutyl-2-dimethylamino-8-hydroxy-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenoxy]-ethoxy}-ethoxy)-ethyl]-triethyl-ammonium iodide Show/Hide	C38H64IN3O6S	1
1	IC50 = 200 nM Bioactivity Info	TI LI LO TS
CP0930732 Compound Info	1-[2-(2-{2-[4-((8R,9R)-7,7-Dibutyl-2-dimethylamino-8-hydroxy-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenoxy]-ethoxy}-ethoxy)-ethyl]-pyridinium iodide Show/Hide	C37H54IN3O6S	1
1	IC50 = 310 nM Bioactivity Info	TI LI LO TS
CP0441440 Compound Info	(8R,9R)-9-(3-Amino-phenyl)-7,7-dibutyl-2-dimethylamino-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C26H39N3O3S	1
1	IC50 = 320 nM Bioactivity Info	TI LI LO TS
CP0918273 Compound Info	{[3-((8R,9R)-7,7-Dibutyl-2-dimethylamino-8-hydroxy-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenylcarbamoyl]-methyl}-triethyl-ammonium chloride Show/Hide	C34H55ClN4O4S	1
1	IC50 = 320 nM Bioactivity Info	TI LI LO TS
CP0451961 Compound Info	(8R,9R)-7,7-Dibutyl-2-dimethylamino-9-(4-methoxy-phenyl)-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C27H40N2O4S	1
1	IC50 = 570 nM Bioactivity Info	TI LI LO TS
CP0498316 Compound Info	(8R,9R)-7,7-Dibutyl-2-dimethylamino-9-(4-hydroxy-phenyl)-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C26H38N2O4S	1
1	IC50 = 580 nM Bioactivity Info	TI LI LO TS
CP0518214 Compound Info	5-Bromo-pentanoic acid [3-((8R,9R)-7,7-dibutyl-2-dimethylamino-8-hydroxy-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenyl]-amide Show/Hide	C31H46BrN3O4S	1
1	IC50 = 690 nM Bioactivity Info	TI LI LO TS
CP0461308 Compound Info	2-Chloro-N-[3-((8R,9R)-7,7-dibutyl-2-dimethylamino-8-hydroxy-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-9-yl)-phenyl]-acetamide Show/Hide	C28H40ClN3O4S	1
1	IC50 = 970 nM Bioactivity Info	TI LI LO TS
CP0507690 Compound Info	(8R,9R)-7,7-Dibutyl-2-dimethylamino-9-(3-methoxy-phenyl)-6-methyl-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C27H40N2O4S	1
1	IC50 = 1200 nM Bioactivity Info	TI LI LO TS
CP0535069 Compound Info	(8R,9R)-7,7-Dibutyl-2-dimethylamino-6-methyl-9-(3-nitro-phenyl)-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C26H37N3O5S	1
1	IC50 = 1200 nM Bioactivity Info	TI LI LO TS
CP0420932 Compound Info	(8R,9R)-6-Benzyl-7,7-dibutyl-2-dimethylamino-9-(3-ethylamino-phenyl)-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C34H47N3O3S	1
1	IC50 = 2500 nM Bioactivity Info	TI LI LO TS
CP0457333 Compound Info	1-(3,4-Dimethoxy-phenyl)-3-(3-ethyl-pentanoyl)-4-hydroxy-6,7,8-trimethoxy-naphthalene-2-carboxylic acid methyl ester Show/Hide	C30H36O9	1
1	IC50 = 2550 nM Bioactivity Info	TI LI LO TS
CP0509796 Compound Info	4-(3,4-Dimethoxy-phenyl)-5,6,7-trimethoxy-3-methyl-2-phenyl-quinoline Show/Hide	C27H27NO5	1
1	IC50 = 3500 nM Bioactivity Info	TI LI LO TS
CP0551285 Compound Info	4-(3,4-Dimethoxy-phenyl)-2-isopropyl-5,6,7-trimethoxy-quinoline-3-carboxylic acid ethyl ester Show/Hide	C26H31NO7	1
1	IC50 = 4400 nM Bioactivity Info	TI LI LO TS
CP0430946 Compound Info	4-(3,4-Dimethoxy-phenyl)-2-ethyl-5,6,7-trimethoxy-3-methyl-quinoline Show/Hide	C23H27NO5	1
1	IC50 = 7100 nM Bioactivity Info	TI LI LO TS
CP0374645 Compound Info	4-(3,4-Dimethoxy-phenyl)-5,6,7-trimethoxy-2-(3-methyl-butyl)-quinoline Show/Hide	C25H31NO5	1
1	IC50 = 9200 nM Bioactivity Info	TI LI LO TS
CP0457332 Compound Info	4-(3,4-Dimethoxy-phenyl)-2-isopropyl-5,6,7-trimethoxy-quinoline Show/Hide	C23H27NO5	1
1	IC50 = 10800 nM Bioactivity Info	TI LI LO TS
CP0514261 Compound Info	4-(3,4-Dimethoxy-phenyl)-2-(3-ethyl-pentyl)-5,6,7-trimethoxy-quinoline-3-carboxylic acid ethyl ester Show/Hide	C30H39NO7	1
1	IC50 = 13300 nM Bioactivity Info	TI LI LO TS
CP0432273 Compound Info	4-(3,4-Dimethoxy-phenyl)-2-(4-fluoro-phenyl)-5,6,7-trimethoxy-quinoline Show/Hide	C26H24FNO5	1
1	IC50 = 49000 nM Bioactivity Info	TI LI LO TS
CP0496229 Compound Info	(8R,9R)-6-Benzyl-7,7-dibutyl-2-dimethylamino-9-(3-nitro-phenyl)-5,5-dioxo-6,7,8,9-tetrahydro-5H-5lambda6-thia-6-aza-benzocyclohepten-8-ol Show/Hide	C32H41N3O5S	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000880 , COS

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000031 , MDCK

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0555899 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepine-8-carbonyl]amino]ethanesulfonic acid Show/Hide	C25H34N2O7S2	1
1	IC50 = 2 nM
CP0139545 Compound Info	3-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]propane-1-sulfonic acid Show/Hide	C25H35NO6S2	1
1	IC50 = 4 nM
CP0403853 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]-2-oxoethanesulfonic acid Show/Hide	C25H34N2O7S2	1
1	IC50 = 9 nM
CP0537937 Compound Info	[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepine-8-carbonyl]amino]methanesulfonic acid Show/Hide	C24H32N2O7S2	1
1	IC50 = 11 nM
CP0351731 Compound Info	[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylphosphonic acid Show/Hide	C23H32NO6PS	1
1	IC50 = 23 nM
CP0224602 Compound Info	3-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepine-8-carbonyl]amino]-2,2-dimethylpropanoic acid Show/Hide	C28H38N2O6S	1
1	IC50 = 32 nM
CP0228144 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methyl-methylamino]acetic acid Show/Hide	C26H36N2O5S	1
1	IC50 = 41 nM
CP0396473 Compound Info	BDBM50434858 Show/Hide	C28H38N2O7S	1
1	IC50 = 43 nM
CP0232120 Compound Info	3-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]propylphosphonic acid Show/Hide	C25H36NO6PS	1
1	IC50 = 51 nM
CP0537934 Compound Info	2-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]ethylphosphonic acid Show/Hide	C24H34NO6PS	1
1	IC50 = 51 nM
CP0394907 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]ethanesulfonic acid Show/Hide	C25H36N2O6S2	1
1	IC50 = 54 nM
CP0435686 Compound Info	(2S)-2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]-3-hydroxypropanoic acid Show/Hide	C26H36N2O6S	1
1	IC50 = 59 nM
CP0395511 Compound Info	3-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]-3-oxopropane-1-sulfonic acid Show/Hide	C26H36N2O7S2	1
1	IC50 = 128 nM
CP0244470 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methyl-(carboxymethyl)amino]acetic acid Show/Hide	C27H36N2O7S	1
1	IC50 = 145 nM
CP0143570 Compound Info	[3-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]propanoylamino]methanesulfonic acid Show/Hide	C26H36N2O7S2	1
1	IC50 = 167 nM
CP0396469 Compound Info	[2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]-2-oxoethyl]phosphonic acid Show/Hide	C25H35N2O7PS	1
1	IC50 = 249 nM
CP0368992 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methyl-(2-sulfoethyl)amino]ethanesulfonic acid Show/Hide	C27H40N2O9S3	1
1	IC50 = 365 nM
CP0407414 Compound Info	(2S,3R)-2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]-3-hydroxybutanoic acid Show/Hide	C27H38N2O6S	1
1	IC50 = 425 nM
CP0396468 Compound Info	(2R)-1-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methyl]pyrrolidine-2-carboxylic acid Show/Hide	C28H38N2O5S	1
1	IC50 = 751 nM
CP0525375 Compound Info	4-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]butanoic acid Show/Hide	C27H38N2O5S	1
1	IC50 = 1287 nM
CP0322547 Compound Info	(2S)-6-amino-2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]hexanoic acid Show/Hide	C29H43N3O5S	1
1	IC50 = 1458 nM
CP0351730 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepine-8-carbonyl]-(carboxymethyl)amino]acetic acid Show/Hide	C27H34N2O8S	1
1	IC50 = 2540 nM
CP0465266 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]ethylphosphonic acid Show/Hide	C25H37N2O6PS	1
1	IC50 = 2698 nM
CP0515313 Compound Info	BDBM50434875 Show/Hide	C30H40N2O8S	1
1	IC50 = 3330 nM
CP0143578 Compound Info	[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]methylphosphonic acid Show/Hide	C24H35N2O6PS	1
1	IC50 = 3360 nM
CP0368993 Compound Info	(2S)-1-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methyl]pyrrolidine-2-carboxylic acid Show/Hide	C28H38N2O5S	1
1	IC50 = 3900 nM
CP0449545 Compound Info	2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]-2-oxoacetic acid Show/Hide	C25H32N2O6S	1
1	IC50 = 8992 nM

Clinical Information about the Protein

Target 1 ( Ileal sodium/bile acid cotransporter (SLC10A2) )

Target Type	Successful Target
Disease	3 Target-related Diseases				3
1	Pruritus [ICD-11: EC90]
2	Hyperlipidaemia [ICD-11: 5C80]
3	Type-2 diabetes [ICD-11: 5A11]
Approved Drug(s)	2 Approved Drugs				2
1	Odevixibat	Drug Info	Approved	Pruritus
2	Maralixibat	Drug Info	Approved	Pruritus
Clinical Trial Drug(s)	4 Clinical Trial Drugs				4
1	264W94	Drug Info	Phase 2	Hyperlipidaemia
2	GSK2330672	Drug Info	Phase 2	Type-2 diabetes
3	S-8921	Drug Info	Phase 2	Hyperlipidaemia
4	Taurocholic Acid	Drug Info	Phase 1/2	Type-2 diabetes

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han