SLC10A2

Summary

SLC10A2 (solute carrier family 10 member 2, HGNC:10906) is a protein-coding gene on chromosome 13q33.1, encoding Ileal sodium/bile acid cotransporter (Q12908). Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine.

This gene encodes a sodium/bile acid cotransporter. This transporter is the primary mechanism for uptake of intestinal bile acids by apical cells in the distal ileum. Bile acids are the catabolic product of cholesterol metabolism, so this protein is also critical for cholesterol homeostasis. Mutations in this gene cause primary bile acid malabsorption (PBAM); muatations in this gene may also be associated with other diseases of the liver and intestines, such as familial hypertriglyceridemia (FHTG).

Source: NCBI Gene 6555 — RefSeq curated summary.

At a glance

• Gene–disease (curated): bile acid malabsorption, primary, 1 (Limited, GenCC)
• GWAS associations: 10
• Clinical variants (ClinVar): 420 total — 1 pathogenic
• Phenotypes (HPO): 8
• Druggable target: yes — 9 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000452

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10906
Approved symbol	SLC10A2
Name	solute carrier family 10 member 2
Location	13q33.1
Locus type	gene with protein product
Status	Approved
Aliases	NTCP2, IBAT
Ensembl gene	ENSG00000125255
Ensembl biotype	protein_coding
OMIM	601295
Entrez	6555

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000245312

RefSeq mRNA: 1 — MANE Select: NM_000452 NM_000452

CCDS: CCDS9506

Canonical transcript exons

ENST00000245312 — 6 exons

Exon	Start	End
ENSE00000854028	103065873	103066417
ENSE00000854029	103058264	103058382
ENSE00000854031	103051257	103051432
ENSE00000854032	103049289	103049446
ENSE00000854033	103043998	103046260
ENSE00000998725	103052620	103052708

Expression profiles

Bgee: expression breadth broad, 49 present calls, max score 97.75.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0648 / max 71.0685, expressed in 14 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
138114	0.0268	7
138116	0.0174	3
138117	0.0119	4
138113	0.0045	1
138115	0.0042	1

Top tissues by expression

267 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
ileal mucosa	UBERON:0000331	97.75	gold quality
jejunal mucosa	UBERON:0000399	86.92	gold quality
duodenum	UBERON:0002114	86.57	gold quality
small intestine Peyer’s patch	UBERON:0003454	85.86	gold quality
nephron tubule	UBERON:0001231	85.68	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	85.28	silver quality
small intestine	UBERON:0002108	82.26	gold quality
kidney epithelium	UBERON:0004819	81.21	gold quality
renal glomerulus	UBERON:0000074	77.89	gold quality
metanephric glomerulus	UBERON:0004736	77.79	gold quality
kidney	UBERON:0002113	66.97	gold quality
cortex of kidney	UBERON:0001225	66.91	gold quality
jejunum	UBERON:0002115	66.10	gold quality
adult mammalian kidney	UBERON:0000082	65.34	gold quality
metanephros	UBERON:0000081	62.54	gold quality
type B pancreatic cell	CL:0000169	62.31	gold quality
cranial nerve II	UBERON:0000941	57.72	silver quality
gall bladder	UBERON:0002110	56.75	gold quality
pancreatic ductal cell	CL:0002079	56.47	silver quality
sural nerve	UBERON:0015488	55.33	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	55.25	silver quality
amniotic fluid	UBERON:0000173	54.63	silver quality
endothelial cell	CL:0000115	54.53	gold quality
epithelial cell of pancreas	CL:0000083	52.51	gold quality
renal medulla	UBERON:0000362	52.43	silver quality
deltoid	UBERON:0001476	52.14	gold quality
quadriceps femoris	UBERON:0001377	50.48	gold quality
frontal pole	UBERON:0002795	50.41	gold quality
middle frontal gyrus	UBERON:0002702	50.30	gold quality
paraflocculus	UBERON:0005351	50.18	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.27

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AP1, CDX2, DNMT1, FOS, HNF1A, JUN, NR0B2, NR1H4, NR3C1, NR5A2, PPARA, RARA, TCFL5

miRNA regulators (miRDB)

101 targeting SLC10A2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-6077	99.99	68.04	2299
HSA-MIR-513B-5P	99.99	69.96	2150
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4500	99.99	72.72	2367
HSA-MIR-223-3P	99.99	70.14	1140
HSA-MIR-4534	99.99	66.58	1907
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-4760-3P	99.93	70.50	2385
HSA-MIR-338-5P	99.92	72.34	2951
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394

Literature-anchored findings (GeneRIF, showing 40)

• There was no apparent correlation between the SLC10A2 polymorphisms and bile acid production or turnover in familial hypertriglyceridemia patients. (PMID:11742882)
• reglation of the ASBT gene by PPARalpha (PMID:12055195)
• role in transport of bile acids in multidrug-resistance-protein 3-overexpressing cells (PMID:12220224)
• Positively regulated by retinoic acid. Bile acids induce negative feedback regulation of human ASBT via farnesoid X-receptor-mediated, short heterodimer partner-dependent effect upon retinoic acid receptor/retinoid X receptor activation of ASBT. (PMID:15239098)
• SLC10A2 expression is regulated by the ubiquitin-proteasome pathway (PMID:15304498)
• On the basis of seven transmembrane topology, a three-dimensional model of ASBT is built. The model agrees with available data for pathological mutation P290S because the mutant model after in silico mutagenesis loses the ability to bind bile acids. (PMID:15350125)
• BIle acid-methanethiosulfonyl can serve as novel and powerful tools to probe the role of endogenous as well as engineered Cys residues in the bile acid binding region(s) of hASBT. (PMID:15952798)
• current data provide the first evidence that I-BABP is functionally associated with FXR and IBAT in the nucleus and on the membrane, respectively, stimulating FXR transcriptional activity and the conjugated bile acid uptake mediated by IBAT in the ileum (PMID:16230354)
• ASBT and ILBP protein were 48% and 67% lower in normal weight gallstone carriers than in controls (P < 0.05); similar differences were found for mRNA expression levels. (PMID:16237211)
• this study determines a 7TM topology for hASBT and refutes the previously proposed 9TM model (PMID:16411770)
• hASBT-mediated prodrug targeting is discussed, including QSAR, in vitro models for hASBT assay, and the current progress in utilizing hASBT as a drug delivery target. (PMID:16749855)
• Although the presence of a single negative charge was not essential for interaction with hASBT, monoanionic conjugates are favored for hASBT-mediated transport compared to cationic and zwitterionic conjugates. (PMID:16749860)
• These data suggest that transmembrane segment 7 (TM7) plays a dominant role in the hASBT translocation process. (PMID:16899538)
• One or more constituents of human serum stimulate ASBT gene expression largely via the down-stream AP-1 response element. (PMID:17942302)
• Extracellular loop 3 amino acids are essential for human ASBT activity as primary substrate interaction points using long-range electrostatic attractive forces. (PMID:18028035)
• cholesterol content of lipid rafts is essential for the optimal activity of ASBT (PMID:18063707)
• involvement of transmembrane domain 4 (TM4) of hASBT in forming the putative translocation pathway. TM4 has distinct helical face that contains residues critical for transport & conformational stability. (PMID:18311924)
• analysis of how conserved aspartic acid residues lining the extracellular loop 1 of sodium-coupled bile acid transporter ASBT interact with Na+ and 7alpha-OH moieties on the ligand cholestane skeleton (PMID:18508772)
• Common variants of the SLC10A2 gene are not associated with sporadic or familial colorectal cancer (PMID:18644122)
• dysfunction, and impaired adaptive responses of several of the bile acid transporters, e.g. BSEP and ASBT, results in liver and intestinal disease (PMID:18668439)
• Cyclic AMP-mediated phosphoinositide-3-kinase{ISBT)-independent activation of Rab4 facilitates Ntcp translocation in a hepatoma cell line. (PMID:18688880)
• haplotype carriers with the minor allele exhibited significant reduced ileal SLC10A2 expression on mRNA levels (2.6-fold, P = 0.0009) and protein levels (2.4-fold, P = 0.0157) (PMID:19184108)
• Integration of results for transmembrane (TM)3 and TM7 cysteine mutants suggests a putative scenario to describe substrate entry and exit into the ASBT permeation pathway during translocation mechanisms. (PMID:19653651)
• SLC10A2 is a novel susceptibility gene for cholelithiasis in humans (PMID:19823678)
• Data demonstrate a novel role of lipid rafts in the modulation of ASBT function by the dietary component EGCG, which may underlie the hypocholesterolemic effects of green tea. (PMID:20056894)
• Results show that bile acid conjugates are potential prolonged release prodrugs with binding affinity for ASBT. (PMID:20600720)
• These data confirm that bile acids and upregulation of ASBT play a crucial role in NEC pathogenesis and suggest that inhibition of ASBT could be utilized as a therapeutic modality against this disease. (PMID:20616306)
• the essential role of ASBT in the uptake of bile acids, by which the enterohepatic recirculation of bile acids is maintained (PMID:21341987)
• The beneficial effect of rifampicin in cholestasis is associated with an increase in DME expression involved in toxic, bile acid and cholesterol metabolism, as well as a reduction in the bile acid importing system in hepatocytes. (PMID:21526375)
• data demonstrate that TM1 plays a pivotal role in ASBT function and stability, thereby providing further insight in its dynamic transport mechanism (PMID:21646357)
• Presence of multiple functionally relevant variants in SLC10A2 that may influence bile acid homeostasis and physiology. (PMID:21649730)
• The human ASBT promoter was activated transcriptionally by CDX1 and CDX2. (PMID:22016432)
• There was no significant association of rs9514089 with gallstone risk, serum lipid parameters and BMI in the Sorbs and in the meta-analysis of all three cohorts. [meta-analysis] (PMID:22093174)
• This study provided novel evidence for the alterations in the activity of ASBT by enteropathogenic Escherichia coli infection. (PMID:22403793)
• ASBT evolved from the earliest vertebrates by gaining affinity for modern bile salts while retaining affinity for older bile salts (PMID:22669917)
• Transmembrane domain II of the human bile acid transporter SLC10A2 coordinates sodium translocation. (PMID:24045943)
• It was conclude that regulation of ASBT expression by resveratrol (RSV) may have clinical relevance with regard to the observed cholesterol-lowering effects of RSV. (PMID:24498857)
• Data indicate that the lipid flippase (ATP8B1)-transmembrane protein 30A (CDC50A) heterodimer is essential for the apical localization of sodium-dependent bile acid transporter (SLC10A2/ASBT) in Caco-2 cells. (PMID:25239307)
• The p.Ser267Phe NTCP variant is significantly associated with resistance to chronic hepatitis B and a lower incidence of acute-on-chronic liver failure. Our results support that NTCP is a cellular receptor for HBV in human infection (PMID:25418280)
• Results unravel novel roles for N-glycosylation of ASBT and suggest that high levels of glucose alter the composition of the glycan and may contribute to the increase in ASBT function in diabetes mellitus. (PMID:25855079)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	slc10a2	ENSDARG00000014916
mus_musculus	Slc10a2	ENSMUSG00000023073
rattus_norvegicus	Slc10a2	ENSRNOG00000037753

Paralogs (5): SLC10A1 (ENSG00000100652), SLC10A3 (ENSG00000126903), SLC10A4 (ENSG00000145248), SLC10A6 (ENSG00000145283), SLC10A5 (ENSG00000253598)

Protein

Protein identifiers

Ileal sodium/bile acid cotransporter — Q12908 (reviewed: Q12908)

Alternative names: 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

All UniProt accessions (1): Q12908

UniProt curated annotations — full annotation on UniProt →

Function. Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine. Transports various bile acids, unconjugated or conjugated, such as cholate and taurocholate. Also responsible for bile acid transport in the renal proximal tubules, a salvage mechanism that helps conserve bile acids. 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.

Subunit / interactions. Monomer and homodimer.

Subcellular location. Membrane.

Tissue specificity. Mainly expressed in ileum and kidney, lower expression in cecum.

Disease relevance. Bile acid malabsorption, primary, 1 (PBAM1) [MIM:613291] An autosomal recessive intestinal disorder associated with chronic watery diarrhea, excess fecal bile acids, steatorrhea and interruption of the enterohepatic circulation of bile acids. The disease is caused by variants affecting the gene represented in this entry.

Similarity. Belongs to the bile acid:sodium symporter (BASS) (TC 2.A.28) family.

RefSeq proteins (1): NP_000443* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002657	BilAc:Na_symport/Acr3	Family
IPR004710	Bilac:Na_transpt	Family
IPR038770	Na+/solute_symporter_sf	Homologous_superfamily

Pfam: PF01758

Catalyzed reactions (Rhea), 9 shown:

• tauroallocholate(out) + 2 Na(+)(out) = tauroallocholate(in) + 2 Na(+)(in) (RHEA:51840)
• taurocholate(out) + 2 Na(+)(out) = taurocholate(in) + 2 Na(+)(in) (RHEA:71875)
• cholate(out) + 2 Na(+)(out) = cholate(in) + 2 Na(+)(in) (RHEA:71911)
• tauronorcholate(out) + 2 Na(+)(out) = tauronorcholate(in) + 2 Na(+)(in) (RHEA:71915)
• taurochenodeoxycholate(out) + 2 Na(+)(out) = taurochenodeoxycholate(in) + 2 Na(+)(in) (RHEA:71923)
• tauroursodeoxycholate(out) + 2 Na(+)(out) = tauroursodeoxycholate(in) + 2 Na(+)(in) (RHEA:71927)
• glycocholate(out) + 2 Na(+)(out) = glycocholate(in) + 2 Na(+)(in) (RHEA:71935)
• taurodeoxycholate(out) + 2 Na(+)(out) = taurodeoxycholate(in) + 2 Na(+)(in) (RHEA:72087)
• tauro-beta-muricholate(out) + 2 Na(+)(out) = tauro-beta-muricholate(in) + 2 Na(+)(in) (RHEA:72179)

UniProt features (29 total): topological domain 8, transmembrane region 7, sequence variant 6, mutagenesis site 2, chain 1, region of interest 1, compositionally biased region 1, site 1, modified residue 1, glycosylation site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q12908-F1	82.88	0.51

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 328 (not glycosylated)

Post-translational modifications (1): 335

Glycosylation sites (1): 10

Mutagenesis-validated functional residues (2):

Position	Phenotype
10	abolishes glycosylation.
328	no effect on glycosylation.

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-159418	Recycling of bile acids and salts

MSigDB gene sets: 142 (showing top): MODULE_162, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_ORGANIC_ACID_TRANSPORT, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, MODULE_368, GATA6_01, BROWNE_HCMV_INFECTION_14HR_DN, GOBP_ORGANIC_ANION_TRANSPORT, MODULE_71, GOBP_BILE_ACID_AND_BILE_SALT_TRANSPORT, TGANTCA_AP1_C, GOBP_MONOCARBOXYLIC_ACID_TRANSPORT, GOCC_APICAL_PLASMA_MEMBRANE, AACTTT_UNKNOWN, RFX1_02

GO Biological Process (6): response to bacterium (GO:0009617), bile acid and bile salt transport (GO:0015721), monoatomic ion transport (GO:0006811), sodium ion transport (GO:0006814), lipid transport (GO:0006869), transmembrane transport (GO:0055085)

GO Molecular Function (3): bile acid:sodium symporter activity (GO:0008508), protein binding (GO:0005515), symporter activity (GO:0015293)

GO Cellular Component (4): plasma membrane (GO:0005886), microvillus (GO:0005902), apical plasma membrane (GO:0016324), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Bile acid and bile salt metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transport	3
response to other organism	1
lipid transport	1
monocarboxylic acid transport	1
organic hydroxy compound transport	1
metal ion transport	1
lipid localization	1
cellular process	1
organic acid:sodium symporter activity	1
bile acid transmembrane transporter activity	1
secondary active monocarboxylate transmembrane transporter activity	1
binding	1
secondary active transmembrane transporter activity	1
membrane	1
cell periphery	1
actin filament bundle	1
actin-based cell projection	1
apical part of cell	1
plasma membrane region	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1166 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLC10A2	FABP6	P51161	916
SLC10A2	NR1H4	Q96RI1	903
SLC10A2	SLC51A	Q86UW1	881
SLC10A2	CYP7A1	P22680	867
SLC10A2	ATP6V0C	P27449	857
SLC10A2	ABCB4	P21439	848
SLC10A2	SLCO1A2	P46721	823
SLC10A2	NR0B2	Q15466	819
SLC10A2	SLC51B	Q86UW2	818
SLC10A2	ABCB11	O95342	802
SLC10A2	PPARA	Q07869	751
SLC10A2	GPBAR1	Q8TDU6	732
SLC10A2	CYP8B1	Q9UNU6	719
SLC10A2	SLC5A1	P13866	685
SLC10A2	FGF19	O95750	671

IntAct

35 interactions, top by confidence:

A	B	Type	Score
SLC10A2	NRM	psi-mi:“MI:0915”(physical association)	0.560
UPK1B	SLC10A2	psi-mi:“MI:0915”(physical association)	0.560
EFNA5	SLC10A2	psi-mi:“MI:0915”(physical association)	0.560
SLC10A2	TTMP	psi-mi:“MI:0915”(physical association)	0.560
SLC10A2	TMEM222	psi-mi:“MI:0915”(physical association)	0.560
SLC10A2	TEX264	psi-mi:“MI:0915”(physical association)	0.560
IFITM3	SLC10A2	psi-mi:“MI:0915”(physical association)	0.560
SLC10A2	CCL4L1	psi-mi:“MI:0915”(physical association)	0.560
SLC10A2	CTXN3	psi-mi:“MI:0915”(physical association)	0.560
SLC10A2	PSENEN	psi-mi:“MI:0915”(physical association)	0.560
SLC10A2	CLPTM1	psi-mi:“MI:0915”(physical association)	0.560
SLC10A2	PPIE	psi-mi:“MI:0915”(physical association)	0.400
SLC10A2	CLGN	psi-mi:“MI:0914”(association)	0.350
SLC10A3	CPD	psi-mi:“MI:0914”(association)	0.350
NRM	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
UPK1B	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
EFNA5	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
TTMP	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
TEX264	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
CCL4L1	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
CTXN3	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
PSENEN	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
TMEM222	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000
IFITM3	SLC10A2	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (31): PPIE (Affinity Capture-MS), SLC10A2 (Two-hybrid), SLC10A2 (Two-hybrid), NRM (Two-hybrid), IFITM3 (Two-hybrid), TEX264 (Two-hybrid), EFNA5 (Two-hybrid), TMEM222 (Two-hybrid), PSENEN (Two-hybrid), CTXN3 (Two-hybrid), CCL4L2 (Two-hybrid), CLPTM1 (Affinity Capture-MS), ACSL6 (Affinity Capture-MS), CLGN (Affinity Capture-MS), CLPTM1 (Affinity Capture-MS)

ESM2 similar proteins: A0A2K2BF92, A0A6P3HVI0, A1L1W9, A2VDL4, A4IHB9, A6QP84, B0JZE1, O35874, P49281, P49282, P53985, P53986, P53987, P53988, P70172, Q03064, Q0IHM1, Q0VA82, Q12908, Q28727, Q2XWK0, Q3KNW5, Q3MHW6, Q3U9N9, Q3UEZ8, Q495M3, Q5BKR2, Q5M7K3, Q5PT56, Q5R6B8, Q5U3U7, Q60414, Q62633, Q63344, Q6DEJ6, Q6GPQ3, Q6NT16, Q6PF45, Q6YBV0, Q70EX6

Diamond homologs: A6QP84, O08705, P09131, P26435, P70172, Q12908, Q14973, Q28727, Q3KNW5, Q3UEZ8, Q4JLT5, Q5PT55, Q5PT56, Q60414, Q62633, Q70EX6, Q7XVB3, Q96EP9, Q9CXB2, P21129, Q0V8N6, Q93YR2, B8BDK4, F4JPW1, O34524, Q1EBV7, Q5VRB2, Q650U0, Q6K739, Q8VYY4, Q8ZKL0, Q5PT54, Q8RXE8

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

420 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	270
Likely benign	99
Benign	14

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
8242	NM_000452.3(SLC10A2):c.584_585+1inv	Pathogenic

SpliceAI

565 predictions. Top by Δscore:

Variant	Effect	Δscore
13:103046256:ATAAA:A	acceptor_gain	1.0000
13:103046257:TAAA:T	acceptor_gain	1.0000
13:103046258:AAA:A	acceptor_gain	1.0000
13:103046258:AAAC:A	acceptor_loss	1.0000
13:103046259:AA:A	acceptor_gain	1.0000
13:103046260:ACTAG:A	acceptor_loss	1.0000
13:103046261:C:CC	acceptor_gain	1.0000
13:103046261:C:T	acceptor_loss	1.0000
13:103047940:AGG:A	donor_gain	1.0000
13:103047957:T:TA	donor_gain	1.0000
13:103049282:T:TA	donor_gain	1.0000
13:103049287:A:AC	donor_gain	1.0000
13:103049287:ACAT:A	donor_gain	1.0000
13:103049288:C:CC	donor_gain	1.0000
13:103049288:CAT:C	donor_gain	1.0000
13:103049288:CATC:C	donor_gain	1.0000
13:103049290:T:TA	donor_gain	1.0000
13:103049447:C:CA	acceptor_loss	1.0000
13:103049448:T:A	acceptor_loss	1.0000
13:103051429:CAAT:C	acceptor_gain	1.0000
13:103049283:CCTTA:C	donor_loss	0.9900
13:103049284:CTT:C	donor_loss	0.9900
13:103049285:TTA:T	donor_loss	0.9900
13:103049286:T:TC	donor_loss	0.9900
13:103049287:ACATC:A	donor_gain	0.9900
13:103049288:CA:C	donor_gain	0.9900
13:103049288:CATCC:C	donor_gain	0.9900
13:103049353:G:GT	donor_gain	0.9900
13:103049442:GGCAC:G	acceptor_gain	0.9900
13:103049444:CAC:C	acceptor_gain	0.9900

AlphaMissense

2279 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
13:103052669:C:T	G179E	0.999
13:103049410:G:C	N266K	0.998
13:103049410:G:T	N266K	0.998
13:103051297:C:A	G241W	0.998
13:103052681:G:C	P175R	0.998
13:103052681:G:T	P175H	0.998
13:103066022:A:C	F76L	0.998
13:103066022:A:T	F76L	0.998
13:103066024:A:G	F76L	0.998
13:103049420:C:T	G263E	0.997
13:103049421:C:A	G263W	0.997
13:103051330:C:G	G230R	0.997
13:103051330:C:T	G230R	0.997
13:103052699:A:G	L169P	0.997
13:103065876:A:G	L125P	0.997
13:103065915:G:A	S112F	0.997
13:103065932:G:C	C106W	0.997
13:103066030:A:G	C74R	0.997
13:103066102:C:G	G50R	0.997
13:103066102:C:T	G50R	0.997
13:103049374:G:C	F278L	0.996
13:103049374:G:T	F278L	0.996
13:103049376:A:G	F278L	0.996
13:103049398:A:C	C270W	0.996
13:103049435:A:T	V258D	0.996
13:103051296:C:T	G241E	0.996
13:103051297:C:G	G241R	0.996
13:103051297:C:T	G241R	0.996
13:103051308:C:T	G237D	0.996
13:103051416:C:T	G201D	0.996

dbSNP variants (sampled 300 via entrez): RS1000040762 (13:103058607 C>T), RS1000277399 (13:103050631 A>C), RS1000343391 (13:103061812 A>C), RS1000375212 (13:103054595 C>A,T), RS1000491346 (13:103054779 T>C), RS1000564277 (13:103049744 C>T), RS1000582070 (13:103050447 C>T), RS1000627387 (13:103044739 G>C), RS1000649649 (13:103059649 G>A), RS1000702808 (13:103065539 C>T), RS1001000579 (13:103059941 G>A), RS1001014772 (13:103045257 C>T), RS1001249775 (13:103064674 T>C), RS1001360084 (13:103060763 T>G), RS1001675457 (13:103043646 T>C)

Disease associations

OMIM: gene MIM:601295 | disease phenotypes: MIM:613291

GenCC curated gene-disease

Disease	Classification	Inheritance
bile acid malabsorption, primary, 1	Limited	Autosomal recessive

Mondo (1): bile acid malabsorption, primary, 1 (MONDO:0013214)

Orphanet (1): NON RARE IN EUROPE: Primary bile acid malabsorption (Orphanet:449262)

HPO phenotypes

8 total (8 of 8 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0001508	Failure to thrive
HP:0001510	Growth delay
HP:0002028	Chronic diarrhea
HP:0002570	Steatorrhea
HP:0002630	Fat malabsorption
HP:0003623	Neonatal onset
HP:0034043	Increased fecal bile acid

GWAS associations

10 associations (top):

Study	Trait	p-value
GCST001179_12	Plasma omega-3 polyunsaturated fatty acid levels (docosapentaenoic acid)	4.000000e-07
GCST001672_4	Esophageal cancer (alcohol interaction)	5.000000e-08
GCST002337_9	Amyotrophic lateral sclerosis (sporadic)	6.000000e-06
GCST003815_99	Late-onset Alzheimer’s disease	5.000000e-08
GCST004068_41	Venous thromboembolism adjusted for sickle cell variant rs77121243-T	5.000000e-06
GCST006295_3	Response to quetiapine in schizophrenia	1.000000e-06
GCST007209_3	Gallstone disease	2.000000e-12
GCST009391_1253	Metabolite levels	2.000000e-06
GCST009568_2	epithelial cell adhesion molecule levels	1.000000e-15
GCST012020_143	Serum metabolite levels	4.000000e-12

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0006809	docosapentaenoic acid measurement
EFO:1001870	late-onset Alzheimers disease
EFO:0004761	uric acid measurement
EFO:0010574	epithelial cell adhesion molecule measurement

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
C567652	Bile Acid Malabsorption, Primary (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2778 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

9 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 290,852 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1551	URSODIOL	4	22,553
CHEMBL160	CYCLOSPORINE	4	168,247
CHEMBL17879	MARALIXIBAT CHLORIDE	4	120
CHEMBL240597	CHENODIOL	4	24,403
CHEMBL272427	TAURURSODIOL	4	4,753
CHEMBL363392	MARALIXIBAT	4	205
CHEMBL406393	DEOXYCHOLIC ACID	4	63,215
CHEMBL2387408	LINERIXIBAT	3	373
CHEMBL412272	TAURODEOXYCHOLIC ACID	2	6,983

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

3 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs2301159	Toxicity	3	docetaxel;thalidomide	Prostatic Neoplasms
rs7319981	Toxicity	4	anthracyclines and related substances	Neoplasms
rs9514091	Toxicity	4	anthracyclines and related substances	Neoplasms

PharmGKB variants

3 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2301159	SLC10A2	3	1.50	1	docetaxel;thalidomide
rs7319981	SLC10A2	4	-1.25	1	anthracyclines and related substances
rs9514091	SLC10A2	4	-1.50	1	anthracyclines and related substances

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: transporter — SLC10 family of sodium-bile acid co-transporters

Most potent curated ligand interactions (5 total), top 5:

Ligand	Action	Affinity	Parameter
odevixibat	Inhibition	9.8	pIC50
maralixibat	Inhibition	9.55	pIC50
elobixibat	Inhibition	8.92	pIC50
SC-435	Inhibition	8.82	pIC50
264W94	Inhibition	7.32	pIC50

Binding affinities (BindingDB)

82 measured of 83 human assays (83 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(2S,3R)-2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,2,5-benzothiadiazepin-8-yl)oxy]acetyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]-3-hydroxybutanoic acid	IC50	0.11 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
(2S)-2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,2,5-benzothiadiazepin-8-yl)oxy]acetyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]-3-methylbutanoic acid	IC50	0.13 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
(2S)-2-[[(2R)-2-[[2-[(3-butyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-3-propyl-2,4-dihydro-1lambda6,5-benzothiazepin-8-yl)oxy]acetyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]butanoic acid	IC50	0.15 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
Odevixibat	IC50	0.16 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
(2S)-2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,2,5-benzothiadiazepin-8-yl)oxy]acetyl]amino]-2-phenylacetyl]amino]butanoic acid	IC50	0.18 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
(2S)-2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,2,5-benzothiadiazepin-8-yl)oxy]acetyl]amino]-2-phenylacetyl]amino]propanoic acid	IC50	0.2 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
(2S)-2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,2,5-benzothiadiazepin-8-yl)oxy]acetyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]propanoic acid	IC50	0.3 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
(2R)-2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,2,5-benzothiadiazepin-8-yl)oxy]acetyl]amino]-2-phenylacetyl]amino]-3-methylsulfanylpropanoic acid	IC50	0.35 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
(2S)-2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,2,5-benzothiadiazepin-8-yl)oxy]acetyl]amino]-2-phenylacetyl]amino]-3-methylbutanoic acid	IC50	0.36 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,2,5-benzothiadiazepin-8-yl)oxy]acetyl]amino]-2-phenylacetyl]amino]acetic acid	IC50	0.45 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
2-[[(3R,5R)-3-butyl-7-(dimethylamino)-3-ethyl-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]acetic acid	IC50	1 nM	US-9040518: Chemical compounds
2-[[(2R)-2-[[2-[(3,3-dibutyl-7-methylsulfanyl-1,1-dioxo-5-phenyl-2,4-dihydro-1lambda6,5-benzothiazepin-8-yl)oxy]acetyl]amino]-2-phenylacetyl]amino]acetic acid	IC50	1.2 nM	US-9694018: IBAT inhibitors for the treatment of liver disease
BDBM50434848	IC50	2 nM	US-9040518: Chemical compounds
2-[[(3R,5R)-3-butyl-3-ethyl-4-hydroxy-7-methoxy-1,1-dioxo-5-phenyl-2,5-dihydro-1lambda6,4-benzothiazepin-8-yl]methylamino]acetic acid	IC50	2 nM	US-9040518: Chemical compounds
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	IC50	2 nM	US-9040518: Chemical compounds
(E)-3-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]prop-2-enoic acid	IC50	3 nM	US-9040518: Chemical compounds
[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methanesulfonic acid	IC50	4 nM	US-9040518: Chemical compounds
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	IC50	4 nM	US-9040518: Chemical compounds
2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]acetic acid	IC50	6 nM	US-9040518: Chemical compounds
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	IC50	6 nM	US-9040518: Chemical compounds
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	IC50	9 nM	US-9040518: Chemical compounds
[[(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	IC50	11 nM	US-9040518: Chemical compounds
(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]-4-methylsulfonylbutanoic acid	IC50	13 nM	US-9040518: Chemical compounds
3-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]propanoic acid	IC50	17 nM	US-9040518: Chemical compounds
2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methyl-hydroxyamino]acetic acid	IC50	17 nM	US-9040518: Chemical compounds
3-[[(3R,5R)-3-butyl-7-(dimethylamino)-3-ethyl-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]pentanedioic acid	IC50	19 nM	US-9040518: Chemical compounds
3-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]-N-methylsulfonylpropanamide	IC50	20 nM	US-9040518: Chemical compounds
2-[(3,3-dibutyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl)methylamino]acetic acid	IC50	21 nM	US-9040518: Chemical compounds
[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylphosphonic acid	IC50	23 nM	US-9040518: Chemical compounds
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	IC50	32 nM	US-9040518: Chemical compounds
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	IC50	41 nM	US-9040518: Chemical compounds
BDBM50434858	IC50	43 nM	US-9040518: Chemical compounds
(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]propanoic acid	IC50	47 nM	US-9040518: Chemical compounds
3-[[(3R,5R)-3-butyl-3-ethyl-4-hydroxy-7-methoxy-1,1-dioxo-5-phenyl-2,5-dihydro-1lambda6,4-benzothiazepin-8-yl]methylamino]pentanedioic acid	IC50	51 nM	US-9040518: Chemical compounds
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	IC50	51 nM	US-9040518: Chemical compounds
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	IC50	51 nM	US-9040518: Chemical compounds
(3,3-dibutyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl)methylphosphonic acid	IC50	52 nM	US-9040518: Chemical compounds
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	IC50	54 nM	US-9040518: Chemical compounds
(2R)-2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]propanoic acid	IC50	55 nM	US-9040518: Chemical compounds
(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	IC50	59 nM	US-9040518: Chemical compounds
(2R)-2-amino-3-[[(2R)-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-carboxyethyl]disulfanyl]propanoic acid	IC50	67 nM	US-9040518: Chemical compounds
3-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]-N-hydroxypropanamide	IC50	68 nM	US-9040518: Chemical compounds
(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepine-8-carboxamide	IC50	73 nM	US-9040518: Chemical compounds
4-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]butanamide	IC50	73 nM	US-9040518: Chemical compounds
BDBM50434845	IC50	100 nM	US-9040518: Chemical compounds
1-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]ethanone	IC50	100 nM	US-9040518: Chemical compounds
[(3R,5R)-3-butyl-3-ethyl-4-hydroxy-7-methoxy-1,1-dioxo-5-phenyl-2,5-dihydro-1lambda6,4-benzothiazepin-8-yl]methylphosphonic acid	IC50	124 nM	US-9040518: Chemical compounds
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	IC50	128 nM	US-9040518: Chemical compounds
[(E)-2-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]ethenyl]phosphonic acid	IC50	131 nM	US-9040518: Chemical compounds
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	IC50	145 nM	US-9040518: Chemical compounds

ChEMBL bioactivities

300 potent at pChembl≥5 of 346 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.55	IC50	0.28	nM	MARALIXIBAT
9.52	IC50	0.3	nM	CHEMBL370103
9.30	IC50	0.5	nM	CHEMBL364676
9.12	IC50	0.76	nM	CHEMBL555246
9.12	IC50	0.75	nM	CHEMBL194685
9.00	IC50	1	nM	CHEMBL372080
9.00	IC50	1	nM	CHEMBL195012
9.00	IC50	1	nM	CHEMBL3658914
8.80	IC50	1.6	nM	CHEMBL332974
8.70	IC50	2	nM	CHEMBL2387421
8.70	IC50	2	nM	CHEMBL2387520
8.70	IC50	2	nM	CHEMBL197508
8.70	IC50	2	nM	CHEMBL540126
8.70	IC50	2	nM	CHEMBL555022
8.70	IC50	2	nM	CHEMBL372324
8.70	IC50	2	nM	CHEMBL193847
8.70	IC50	2	nM	CHEMBL372275
8.70	IC50	2	nM	CHEMBL3959109
8.70	IC50	2	nM	CHEMBL3658886
8.70	IC50	2	nM	CHEMBL3658901
8.66	IC50	2.2	nM	CHEMBL194461
8.64	IC50	2.3	nM	CHEMBL196032
8.62	IC50	2.4	nM	CHEMBL3956446
8.52	IC50	3	nM	CHEMBL555024
8.52	IC50	3	nM	CHEMBL611748
8.52	IC50	3	nM	CHEMBL3658876
8.52	IC50	3	nM	CHEMBL332973
8.46	IC50	3.5	nM	CHEMBL3907170
8.44	IC50	3.6	nM	CHEMBL196459
8.43	IC50	3.7	nM	CHEMBL426152
8.40	IC50	4	nM	CHEMBL2387397
8.40	IC50	4	nM	CHEMBL2387522
8.40	IC50	4	nM	CHEMBL2387521
8.40	IC50	4	nM	CHEMBL2387527
8.40	IC50	4	nM	CHEMBL194420
8.40	IC50	4	nM	CHEMBL380601
8.40	IC50	4	nM	CHEMBL196029
8.40	IC50	4	nM	CHEMBL193439
8.40	IC50	4	nM	CHEMBL3658874
8.36	IC50	4.4	nM	CHEMBL3945133
8.35	IC50	4.5	nM	CHEMBL197311
8.30	IC50	5	nM	CHEMBL196475
8.30	IC50	5	nM	CHEMBL194792
8.30	IC50	5	nM	CHEMBL197639
8.24	IC50	5.7	nM	CHEMBL540128
8.22	IC50	6	nM	CHEMBL2387510
8.22	IC50	6	nM	CHEMBL196280
8.22	IC50	6	nM	CHEMBL3658888
8.22	IC50	6	nM	CHEMBL3658910
8.22	IC50	6	nM	CHEMBL122498

PubChem BioAssay actives

220 with measured affinity, of 337 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
2-[[2-[3-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]anilino]acetyl]amino]acetic acid	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0003	uM
Maralixibat	1954580: Inhibition of human IBAT	ic50	0.0003	uM
(4R,5R)-5-[4-[5-(4-aza-1-azoniabicyclo[2.2.2]octan-1-yl)pentoxy]phenyl]-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0005	uM
[5-[3-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]anilino]-5-oxopentyl]-triethylazanium bromide	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0008	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-[4-[(1-methylpyridin-1-ium-4-yl)methoxy]phenyl]-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0008	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-5-[4-[[4-(pyridin-1-ium-1-ylmethyl)phenyl]methoxy]phenyl]-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0010	uM
(4R,5R)-5-[4-[4-(4-aza-1-azoniabicyclo[2.2.2]octan-1-yl)butoxy]phenyl]-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0010	uM
[5-[3-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6,2-benzothiazepin-5-yl]anilino]-5-oxopentyl]-triethylazanium;2,2,2-trifluoroacetate	38743: In vitro inhibitory activity against uptake of [14C]taurocholate in baby hamster kidney cells transfected with cDNA from human Apical Sodium-Codependent Bile Acid Transporter	ic50	0.0016	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-9-methoxy-5-(4-methoxyphenyl)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255078: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in Baby hamster cells expressing human IBAT	ic50	0.0020	uM
5-[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]pentyl-triethylazanium bromide	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0020	uM
5-[3-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]pentyl-triethylazanium bromide	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0020	uM
4-[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]butanoic acid	750716: Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	ic50	0.0020	uM
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	750716: Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	ic50	0.0020	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-[3-[(1-methylpyridin-1-ium-4-yl)amino]phenyl]-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0020	uM
(4R,5R)-5-(3-aminophenyl)-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0020	uM
2-[carboxymethyl-[[4-[[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]methyl]phenyl]methyl]amino]acetic acid	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0020	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-(4-hydroxyphenyl)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0022	uM
2-[carboxymethyl-[5-[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]pentyl]amino]acetic acid	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0023	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-[3-fluoro-4-[2-[2-[2-(4,8,11-trimethyl-1,4,8,11-tetrazacyclotetradec-1-yl)ethoxy]ethoxy]ethoxy]phenyl]-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0030	uM
2-[2-[2-[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6,2-benzothiazepin-5-yl]phenoxy]ethoxy]ethoxy]ethyl-triethylazanium iodide	38743: In vitro inhibitory activity against uptake of [14C]taurocholate in baby hamster kidney cells transfected with cDNA from human Apical Sodium-Codependent Bile Acid Transporter	ic50	0.0030	uM
2-[2-[2-[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]ethoxy]ethoxy]ethyl-triethylazanium bromide	255078: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in Baby hamster cells expressing human IBAT	ic50	0.0030	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-(3-fluoro-4-methoxyphenyl)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0036	uM
[3-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenyl]methanesulfonic acid	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0037	uM
2-[carboxymethyl-[[6-[[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]methyl]-2-pyridinyl]methyl]amino]acetic acid	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0040	uM
2-[2-[2-[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]ethoxy]ethoxy]ethyl-trimethylazanium	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0040	uM
(4R,5R)-5-[4-[2-[2-[2-(4-aza-1-azoniabicyclo[2.2.2]octan-1-yl)ethoxy]ethoxy]ethoxy]phenyl]-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0040	uM
2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methylamino]acetic acid	750716: Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	ic50	0.0040	uM
[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]methanesulfonic acid	750716: Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	ic50	0.0040	uM
2-[[(3R,5R)-3-butyl-3-ethyl-7-methoxy-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6,4-benzothiazepin-8-yl]oxy]ethanesulfonic acid	750716: Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	ic50	0.0040	uM
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	750716: Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	ic50	0.0040	uM
(4R,5R)-5-[4-[3-(4-aza-1-azoniabicyclo[2.2.2]octan-1-yl)propoxy]phenyl]-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0040	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-[3-(hydroxymethyl)phenyl]-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0045	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-5-thiophen-3-yl-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0050	uM
(4R,5S)-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-5-pyridin-2-yl-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0050	uM
(3S,4R,5R)-3-butyl-7-(dimethylamino)-3-ethyl-1,1-dioxo-5-phenyl-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255078: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in Baby hamster cells expressing human IBAT	ic50	0.0050	uM
2-[2-[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]ethoxy]ethyl-triethylazanium bromide	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0057	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-[4-[(1-ethylpyridin-1-ium-4-yl)methoxy]phenyl]-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0060	uM
(4R,5R)-5-(3-aminophenyl)-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2H-1lambda6,2-benzothiazepin-4-ol	38743: In vitro inhibitory activity against uptake of [14C]taurocholate in baby hamster kidney cells transfected with cDNA from human Apical Sodium-Codependent Bile Acid Transporter	ic50	0.0060	uM
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	750716: Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	ic50	0.0060	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-(4-methoxyphenyl)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0068	uM
methyl 3-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]benzoate	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0070	uM
2-[3-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]ethyl-triethylazanium bromide	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0070	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-(3-hydroxyphenyl)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0073	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-5-pyridin-3-yl-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0075	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-5-[3-(pyridin-1-ium-1-ylmethyl)phenyl]-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0075	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-5-pyridin-4-yl-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0080	uM
(4R,5R)-3,3-dibutyl-7-(dimethylamino)-5-(4-hydroxyphenyl)-1,1-dioxo-4,5-dihydro-2H-1lambda6,2-benzothiazepin-4-ol	38743: In vitro inhibitory activity against uptake of [14C]taurocholate in baby hamster kidney cells transfected with cDNA from human Apical Sodium-Codependent Bile Acid Transporter	ic50	0.0080	uM
(4R,5R)-5-[4-[2-[2-(4-aza-1-azoniabicyclo[2.2.2]octan-1-yl)ethoxy]ethoxy]phenyl]-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0085	uM
5-[4-[(4R,5R)-3,3-dibutyl-7-(dimethylamino)-4-hydroxy-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-5-yl]phenoxy]pentanoic acid	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0085	uM
(4R,5R)-5-[4-[2-[2-[2-[bis(2-hydroxyethyl)amino]ethoxy]ethoxy]ethoxy]phenyl]-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2H-1lambda6-benzothiepin-4-ol	255086: In vitro inhibition of ASBT mediated uptake of [14C]taurocholate (5 uM) in baby hamster cells expressing human IBAT	ic50	0.0090	uM

CTD chemical–gene interactions

34 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
deoxynivalenol	decreases expression, decreases reaction	2
Benzo(a)pyrene	affects methylation, increases expression	2
Chenodeoxycholic Acid	decreases reaction, increases transport, increases uptake	2
Taurocholic Acid	increases uptake, decreases reaction, increases transport	2
betulin	affects reaction, increases uptake	1
perfluorooctanoic acid	affects methylation	1
glycoursodeoxycholic acid	decreases reaction, increases uptake	1
ursodoxicoltaurine	increases uptake, decreases reaction	1
cholylsarcosine	increases uptake, decreases reaction	1
lactacystin	decreases expression, decreases reaction	1
benzyloxycarbonylleucyl-leucyl-leucine aldehyde	decreases expression, decreases reaction	1
perfluorooctane sulfonic acid	increases transport	1
SB 203580	decreases expression, decreases reaction	1
2-palmitoylglycerol	increases expression	1
GW 4064	decreases expression, decreases reaction	1
LDN 57444	decreases expression, decreases reaction	1
Resveratrol	decreases expression, decreases reaction, decreases activity	1
Troglitazone	decreases reaction, increases uptake	1
Betulinic Acid	affects reaction, increases uptake	1
Bile Acids and Salts	affects transport	1
Calcitriol	increases expression	1
Deoxycholic Acid	increases uptake, decreases reaction	1
Erythrosine	decreases reaction, increases uptake	1
Glycochenodeoxycholic Acid	decreases reaction, increases uptake	1
Glycocholic Acid	increases uptake, decreases reaction	1
Glycodeoxycholic Acid	decreases reaction, increases uptake	1
Indocyanine Green	increases uptake	1
Sodium	decreases reaction, increases uptake	1
Sulfobromophthalein	decreases reaction, increases uptake	1
Taurochenodeoxycholic Acid	increases uptake, decreases reaction	1

ChEMBL screening assays

47 unique, capped per target: 28 binding, 19 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1177270	Binding	Inhibition of human ASBT expressed in MDCK cells assessed as inhibition of [3H]taurocholic acid uptake after 10 mins by liquid scintillation counting	Molecular switch controlling the binding of anionic bile acid conjugates to human apical sodium-dependent bile acid transporter. — J Med Chem
CHEMBL2075351	Functional	TP_TRANSPORTER: uptake in ASBT-expressing HEK293 cells	Identification of a region of the ileal-type sodium/bile acid cotransporter interacting with a competitive bile acid transport inhibitor. — Biochemistry

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.