SCARB1

gene
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Also known as SRB1CLA-1CLA1SR-BI

Summary

SCARB1 (scavenger receptor class B member 1, HGNC:1664) is a protein-coding gene on chromosome 12q24.31, encoding Scavenger receptor class B member 1 (Q8WTV0). Receptor for different ligands such as phospholipids, cholesterol ester, lipoproteins, phosphatidylserine and apoptotic cells.

The protein encoded by this gene is a plasma membrane receptor for high density lipoprotein cholesterol (HDL). The encoded protein mediates cholesterol transfer to and from HDL. In addition, this protein is a receptor for hepatitis C virus glycoprotein E2 and facilitates cell entry by the virus, SARS-CoV2.

Source: NCBI Gene 949 — RefSeq curated summary.

At a glance

  • GWAS associations: 66
  • Clinical variants (ClinVar): 204 total — 1 pathogenic
  • Druggable target: yes — 2 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_005505

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:1664
Approved symbolSCARB1
Namescavenger receptor class B member 1
Location12q24.31
Locus typegene with protein product
StatusApproved
AliasesSRB1, CLA-1, CLA1, SR-BI
Ensembl geneENSG00000073060
Ensembl biotypeprotein_coding
OMIM601040
Entrez949

Gene structure

Transcript identifiers

Ensembl transcripts: 45 — 31 protein_coding, 6 retained_intron, 5 nonsense_mediated_decay, 3 protein_coding_CDS_not_defined

ENST00000261693, ENST00000339570, ENST00000415380, ENST00000535005, ENST00000538291, ENST00000539320, ENST00000541661, ENST00000544327, ENST00000545305, ENST00000545493, ENST00000546215, ENST00000679605, ENST00000679955, ENST00000680556, ENST00000680596, ENST00000680926, ENST00000680982, ENST00000681117, ENST00000681499, ENST00000681555, ENST00000681686, ENST00000681788, ENST00000877826, ENST00000877827, ENST00000877828, ENST00000877829, ENST00000877830, ENST00000877831, ENST00000877832, ENST00000877833, ENST00000877834, ENST00000877835, ENST00000877836, ENST00000877837, ENST00000936307, ENST00000936308, ENST00000936309, ENST00000936310, ENST00000936311, ENST00000936312, ENST00000964690, ENST00000964691, ENST00000964692, ENST00000964693, ENST00000964694

RefSeq mRNA: 11 — MANE Select: NM_005505 NM_001082959, NM_001367981, NM_001367982, NM_001367983, NM_001367984, NM_001367985, NM_001367986, NM_001367987, NM_001367988, NM_001367989, NM_005505

CCDS: CCDS45008, CCDS91769, CCDS91770, CCDS91771, CCDS9259

Canonical transcript exons

ENST00000261693 — 13 exons

ExonStartEnd
ENSE00001329956124863595124863864
ENSE00003474911124811870124811965
ENSE00003524630124800124124800242
ENSE00003526102124810174124810289
ENSE00003544724124814973124815114
ENSE00003577732124782683124782811
ENSE00003581233124787406124787457
ENSE00003607572124795195124795268
ENSE00003608768124786357124786503
ENSE00003635066124807761124807927
ENSE00003673083124817550124817707
ENSE00003678576124814202124814405
ENSE00003681386124776856124778586

Expression profiles

Bgee: expression breadth ubiquitous, 244 present calls, max score 99.70.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 81.3898 / max 6282.2535, expressed in 1790 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter IDTPM avgSamples expressed
13403558.63291727
13403712.48311672
1340386.66091671
1340363.61301323

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
right adrenal gland cortexUBERON:003582799.70gold quality
right adrenal glandUBERON:000123399.68gold quality
left adrenal glandUBERON:000123499.68gold quality
adrenal cortexUBERON:000123599.67gold quality
adrenal tissueUBERON:001830399.66gold quality
left adrenal gland cortexUBERON:003582599.65gold quality
adrenal glandUBERON:000236999.44gold quality
right lobe of liverUBERON:000111498.64gold quality
liverUBERON:000210796.60gold quality
left ovaryUBERON:000211996.26gold quality
right ovaryUBERON:000211896.03gold quality
putamenUBERON:000187495.64gold quality
caudate nucleusUBERON:000187395.44gold quality
omental fat padUBERON:001041495.42gold quality
peritoneumUBERON:000235895.36gold quality
adipose tissue of abdominal regionUBERON:000780895.14gold quality
subcutaneous adipose tissueUBERON:000219094.90gold quality
placentaUBERON:000198794.56gold quality
adipose tissueUBERON:000101393.82gold quality
nucleus accumbensUBERON:000188293.79gold quality
right frontal lobeUBERON:000281093.11gold quality
C1 segment of cervical spinal cordUBERON:000646992.81gold quality
gall bladderUBERON:000211092.78gold quality
connective tissueUBERON:000238492.70gold quality
ovaryUBERON:000099292.32gold quality
duodenumUBERON:000211492.26gold quality
amygdalaUBERON:000187692.18gold quality
pigmented layer of retinaUBERON:000178291.65gold quality
retinaUBERON:000096691.62gold quality
stromal cell of endometriumCL:000225591.47gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-ANND-3yes10.55
E-MTAB-10137no496.59
E-GEOD-81383no158.48

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CREB1, CUX1, DGKQ, ESR1, FOXO1, GLI1, HNF4A, IRF6, KLF4, KMT2A, KMT2B, MSR1, MYC, NR0B2, NR1H2, NR1H3, NR1H4, NR1I2, NR3C1, NR5A1, NR5A2, PPARA, PPARG, PREB, RXRA, SP1, SP3, SPI1, SREBF1, SREBF2, STAT1, STAT2

miRNA regulators (miRDB)

43 targeting SCARB1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-6867-5P100.0082.213464
HSA-MIR-223-3P99.9970.141140
HSA-MIR-4482-3P99.9872.503147
HSA-MIR-4650-5P99.9864.69999
HSA-MIR-96-5P99.9572.802140
HSA-MIR-185-3P99.9567.011743
HSA-MIR-335-3P99.9373.364958
HSA-MIR-345-3P99.8970.231421
HSA-MIR-431999.7669.832586
HSA-MIR-3934-3P99.7665.511351
HSA-MIR-556-3P99.7468.751203
HSA-MIR-430699.7270.503630
HSA-MIR-670-5P99.6769.941565
HSA-MIR-24-3P99.5969.971934
HSA-MIR-3682-3P99.5867.63865
HSA-MIR-766-5P99.4767.912225
HSA-MIR-125A-5P99.3670.591640
HSA-MIR-125B-5P99.3670.361662
HSA-MIR-428499.3665.251293
HSA-MIR-149-5P99.2567.161315
HSA-MIR-4685-5P99.2565.991563
HSA-MIR-6837-5P99.2565.471632
HSA-MIR-66199.0965.942062
HSA-MIR-328-5P99.0864.651000
HSA-MIR-939-3P98.9765.072347
HSA-MIR-455-3P98.9467.68878
HSA-MIR-93698.8770.511124
HSA-MIR-4755-3P98.7765.591915
HSA-MIR-6885-5P98.7164.33902
HSA-MIR-6811-3P98.6266.54944

Literature-anchored findings (GeneRIF, showing 40)

  • binding to high density lipoprotein activates endothelial nitric-oxide synthase in a ceramide-dependent manner (PMID:11792700)
  • SR-BI is a phagocytosis-inducing PS receptor of Sertoli cells. (PMID:12016218)
  • PDZK1 or other PDZ domain proteins may play an important role in regulating SR-BI cell surface expression and hence reverse cholesterol transport. (PMID:12119305)
  • SR-BI regulation of cholesteryl ester uptake is affected by binding to APOE in human cells (PMID:12138091)
  • EDL mediates both HDL binding and uptake, and the selective uptake of HDL-CE, independently of lipolysis and CLA-1. (PMID:12164779)
  • Testosterone up-regulates scavenger receptor BI mRNA in macrophages (PMID:12207878)
  • There is an association between HaeIII polymorphism of scavenger receptor class B type I gene and plasma HDL-cholesterol concentration in patients with CAD. (PMID:12227853)
  • basal and SR-BI-stimulated free cholesterol efflux to HDL and liposomes and SR-BI-mediated selective uptake of HDL cholesteryl ester are not affected by caveolin-1 expression (PMID:12562842)
  • binds and internalizes lipopolysasccharides and lipoproteins and is a orthologue of rodent SR-BI (PMID:12651854)
  • carriers of the minority allele, 1/2, of the scavenger receptor class B type I gene are more susceptible to the presence of saturated fatty acids in the diet because of a greater increase in LDL cholesterol (PMID:12663276)
  • Transcriptional activation of SR-BI is stimulated by peroxisome proliferator-activated receptor gamma and hepatocyte nuclear factor 4alpha. (PMID:12763030)
  • SR-BI gene variation modulates the lipid profile, particularly in type 2 diabetes, contributing to the metabolic abnormalities. (PMID:12788901)
  • Genetic variants in the HDL receptor, SR-B1, may be an important determinant of abnormal lipoproteins in women and may confer particular susceptibility to coronary artery disease. (PMID:12807968)
  • SR-B1 is required for hepatitis C virus infection of CD81-expressing hepatic cells (PMID:12913001)
  • CD36 and SR-BI are receptors for hypochlorite-modified low density lipoprotein (PMID:12968020)
  • Polymorphisms of the HDL receptor gene associated with HDL cholesterol levels in diabetic kindred (PMID:14566094)
  • human intestine possesses a developmental and regional SR-BI pattern of distribution (PMID:14676281)
  • SR-BI-facilitated diffusion is not dependent on pre-beta-high density lipoprotein interaction with human chymase (PMID:14701812)
  • SR-BI-mediated cholesteryl ester-selective uptake and efflux of unesterified cholesterol is regulated by HDL (PMID:14718538)
  • alternative spliced sr-bI (SR-BII) may influence cellular cholesterol trafficking and homeostasis in a manner that is distinct from SR-BI. (PMID:14726519)
  • SR-BI levels in macrophages are responsive to changes in intracellular sterol content and that these sterol-associated changes are not mediated by LXR and are unlikely to be mediated by an SREBP pathway (PMID:14967816)
  • plays a major role in the clearance of apoptotic cells from the thymus. (PMID:15072554)
  • The reciprocal inhibition of SR-BI and ABCA1 by BLT-4 and glyburide raises the possibility that these proteins may share similar or common steps in their mechanisms of lipid transport. (PMID:15102890)
  • Scavenger receptor BI function is not only crucial for cholesterol delivery to the liver but is also important for cholesterol efflux at the vessel wall [review]. (PMID:15166784)
  • SR-BI is associated with membrane rafts devoid of caveolin and its expression affects intracellular lipid binding and lipid sensor proteins in HepG2 cells (PMID:15226391)
  • uptake of lipoprotein-associated phosphatidylcholine by the cerebrovasculature via scavenger receptor class B, type I could generate a pool of lipids (PMID:15342124)
  • endogenous expression of SR-BI/CLA-1 was suppressed by exposure to growth hormone or IGF-I in cultured HepG2 cells (PMID:15345670)
  • SR-B1 is not required for apolipoprotein A-1-mediated endothelial cholesterol efflux from vascular endothelial cells. (PMID:15492319)
  • analysis of uptake of individual HDL particles in living cells via the scavenger receptor class B type I (PMID:15509885)
  • SR-BI plays a key role in SAA metabolism through its ability to interact with and internalize SAA and SAA influences HDL cholesterol metabolism through its inhibitory effects on SR-BI-mediated selective lipid uptake (PMID:15561721)
  • CLA-1 functions as an endocytic SAA receptor and is involved in SAA-mediated cell signaling events associated with the immune-related and inflammatory effects of SAA (PMID:15576377)
  • HDL-mediated enhancement of HCVpp entry involves a complex interplay between SR-BI, HDL, and HCV envelope glycoproteins (PMID:15632171)
  • plausible genetic interaction between the CLA-1 exon 8 gene polymorphism and the risk of coroanry heart disease in males (PMID:15681296)
  • at low levels of high density lipoproteins, oxidative stress causes the relocation of eNOS away from caveolae, which turns on SR-BI-induced apoptosis and rapidly clears damaged cells to prevent further inflammatory damage to neighboring cells (PMID:15749707)
  • SR-BI is expressed in a cell-specific fashion in the initial & terminal steps of reverse cholesterol transport. It may be physiologically relevant and have distinct tissue-specific functions. (PMID:15970294)
  • SR-BI is expressed in a cell-specific fashion in the initial & terminal steps of reverse cholesterol transport. It may be physiologically relevant and have distinct tissue-specific functions. (PMID:15979078)
  • Serum amyloid A has a role in promoting cholesterol efflux mediated by scavenger receptor B-I (PMID:16120612)
  • SR-BI-mediated supply of cholesterol, the substrate for bile acid synthesis. (PMID:16168958)
  • only lipid-bound apoE promotes SR-BI-mediated cholesterol efflux and that the amino-terminal region of residues 1-165 of apoE is sufficient for both receptor binding and cholesterol efflux (PMID:16185081)
  • vitamin E intestinal absorption is, at least in part, mediated by SR-BI (PMID:16380385)

Cross-species orthologs

8 orthologs

OrganismSymbolGene ID
danio_rerioscarb1ENSDARG00000101557
mus_musculusScarb1ENSMUSG00000037936
rattus_norvegicusScarb1ENSRNOG00000000981
drosophila_melanogasterempFBGN0010435
drosophila_melanogasterCG10345FBGN0027562
drosophila_melanogasterCG3829FBGN0035091
drosophila_melanogasterdsbFBGN0035290
drosophila_melanogasterCG40006FBGN0058006

Paralogs (2): CD36 (ENSG00000135218), SCARB2 (ENSG00000138760)

Protein

Protein identifiers

Scavenger receptor class B member 1Q8WTV0 (reviewed: Q8WTV0)

Alternative names: CD36 and LIMPII analogous 1, CD36 antigen-like 1, Collagen type I receptor, thrombospondin receptor-like 1, SR-BI

All UniProt accessions (10): Q8WTV0, A0A0S2Z3I2, A0A7P0T913, A0A7P0T9B3, A0A7P0T9I2, A0A7P0Z4E3, A0A7P0Z4J8, B7ZKQ9, F5H4X0, F5H5E8

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for different ligands such as phospholipids, cholesterol ester, lipoproteins, phosphatidylserine and apoptotic cells. Receptor for HDL, mediating selective uptake of cholesteryl ether and HDL-dependent cholesterol efflux. Also facilitates the flux of free and esterified cholesterol between the cell surface and apoB-containing lipoproteins and modified lipoproteins, although less efficiently than HDL. May be involved in the phagocytosis of apoptotic cells, via its phosphatidylserine binding activity. (Microbial infection) Acts as a receptor for hepatitis C virus in hepatocytes and appears to facilitate its cell entry. Binding between SCARB1 and the hepatitis C virus glycoprotein E2 is independent of the genotype of the viral isolate. (Microbial infection) Mediates uptake of M.fortuitum, E.coli and S.aureus. (Microbial infection) Facilitates the entry of human coronavirus SARS-CoV-2 by acting as an entry cofactor through HDL binding.

Subunit / interactions. The C-terminal region binds to PDZK1. (Microbial infection) Interacts with hepatitis C virus E1:E2 glycoproteins.

Subcellular location. Cell membrane. Membrane. Caveola.

Tissue specificity. Widely expressed.

Post-translational modifications. N-glycosylated. The six cysteines of the extracellular domain are all involved in intramolecular disulfide bonds.

Polymorphism. Genetic variations in SCARB1 define the high density lipoprotein cholesterol level quantitative trait locus 6 (HDLCQ16) [MIM:610762].

Miscellaneous. May be due to a competing donor splice site.

Similarity. Belongs to the CD36 family.

Isoforms (5)

UniProt IDNamesCanonical?
Q8WTV0-13yes
Q8WTV0-21, SR-BI
Q8WTV0-32, SR-BII
Q8WTV0-44, SR-BIII
Q8WTV0-55, SR-BI.2, SR-BII

RefSeq proteins (11): NP_001076428, NP_001354910, NP_001354911, NP_001354912, NP_001354913, NP_001354914, NP_001354915, NP_001354916, NP_001354917, NP_001354918, NP_005496* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR002159CD36_famFamily
IPR005428CD36/SCARB1/SNMP1Family

Pfam: PF01130

UniProt features (33 total): glycosylation site 9, sequence variant 7, splice variant 4, topological domain 3, modified residue 3, transmembrane region 2, sequence conflict 2, chain 1, disulfide bond 1, lipid moiety-binding region 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q8WTV0-F184.250.65

Functional residue map

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

Post-translational modifications (4): 493, 393, 458, 462

Disulfide bonds (1): 251–384

Glycosylation sites (9): 212, 227, 255, 310, 330, 383, 102, 108, 173

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

IDPathway
R-HSA-3000471Scavenging by Class B Receptors
R-HSA-8964011HDL clearance

MSigDB gene sets: 0 (showing top):

GO Biological Process (33): endothelial cell proliferation (GO:0001935), cholesterol catabolic process (GO:0006707), positive regulation of endothelial cell migration (GO:0010595), obsolete positive regulation of nitric oxide mediated signal transduction (GO:0010750), positive regulation of triglyceride biosynthetic process (GO:0010867), positive regulation of cholesterol storage (GO:0010886), regulation of phosphatidylcholine catabolic process (GO:0010899), phospholipid transport (GO:0015914), lipopolysaccharide transport (GO:0015920), detection of lipopolysaccharide (GO:0032497), cholesterol efflux (GO:0033344), high-density lipoprotein particle remodeling (GO:0034375), plasma lipoprotein particle clearance (GO:0034381), low-density lipoprotein particle clearance (GO:0034383), high-density lipoprotein particle clearance (GO:0034384), vitamin transmembrane transport (GO:0035461), wound healing (GO:0042060), vasodilation (GO:0042311), cholesterol homeostasis (GO:0042632), blood vessel endothelial cell migration (GO:0043534), recognition of apoptotic cell (GO:0043654), reverse cholesterol transport (GO:0043691), adhesion of symbiont to host (GO:0044406), regulation of phagocytosis (GO:0050764), high density lipoprotein particle mediated signaling (GO:0055097), triglyceride homeostasis (GO:0070328), cholesterol import (GO:0070508), intestinal lipid absorption (GO:0098856), positive regulation of sphingolipid mediated signaling pathway (GO:1902070), lipid transport (GO:0006869), cholesterol transport (GO:0030301), lipopolysaccharide-mediated signaling pathway (GO:0031663), symbiont entry into host cell (GO:0046718)

GO Molecular Function (14): lipopolysaccharide binding (GO:0001530), amyloid-beta binding (GO:0001540), virus receptor activity (GO:0001618), phosphatidylserine binding (GO:0001786), lipopolysaccharide immune receptor activity (GO:0001875), scavenger receptor activity (GO:0005044), 1-phosphatidylinositol binding (GO:0005545), high-density lipoprotein particle binding (GO:0008035), lipid binding (GO:0008289), low-density lipoprotein particle binding (GO:0030169), apolipoprotein binding (GO:0034185), apolipoprotein A-I binding (GO:0034186), high-density lipoprotein particle receptor activity (GO:0070506), protein binding (GO:0005515)

GO Cellular Component (9): lysosome (GO:0005764), lysosomal membrane (GO:0005765), plasma membrane (GO:0005886), caveola (GO:0005901), cell surface (GO:0009986), endocytic vesicle membrane (GO:0030666), extracellular exosome (GO:0070062), cytoplasm (GO:0005737), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
Binding and Uptake of Ligands by Scavenger Receptors1
Plasma lipoprotein clearance1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
endothelial cell migration2
lipid transport2
plasma lipoprotein particle clearance2
phospholipid binding2
lipoprotein particle binding2
binding2
epithelial cell proliferation1
cholesterol metabolic process1
sterol catabolic process1
alcohol catabolic process1
regulation of endothelial cell migration1
positive regulation of cell migration1
regulation of triglyceride biosynthetic process1
triglyceride biosynthetic process1
positive regulation of lipid biosynthetic process1
positive regulation of triglyceride metabolic process1
cholesterol storage1
positive regulation of lipid storage1
regulation of cholesterol storage1
phosphatidylcholine catabolic process1
regulation of phospholipid catabolic process1
regulation of phosphatidylcholine metabolic process1
organophosphate ester transport1
carbohydrate derivative transport1
detection of molecule of bacterial origin1
response to lipopolysaccharide1
cholesterol transport1
plasma lipoprotein particle remodeling1
receptor-mediated endocytosis1
multicellular organismal process1
plasma lipoprotein particle disassembly1
regulation of plasma lipoprotein particle levels1
low-density lipoprotein particle disassembly1
vitamin transport1
transmembrane transport1
response to wounding1
tissue regeneration1
blood vessel diameter maintenance1
sterol homeostasis1

Protein interactions and networks

STRING

5200 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
SCARB1APOA1P02647998
SCARB1TLR4O00206997
SCARB1TLR2O60603996
SCARB1CD81P18582995
SCARB1THBS1P07996994
SCARB1CD47Q08722994
SCARB1TLR6Q9Y2C9993
SCARB1APOBP04114990
SCARB1LYNP07948973
SCARB1APOEP02649963
SCARB1THBS2P35442950
SCARB1FYNP06241941
SCARB1TLR1Q15399941
SCARB1CLDN1O95832934
SCARB1ABCA1O95477933
SCARB1NPC1L1Q9UHC9933

IntAct

98 interactions, top by confidence:

ABTypeScore
CFTRESYT2psi-mi:“MI:2364”(proximity)0.710
SCARB1reppsi-mi:“MI:0915”(physical association)0.660
CANXPGRMC1psi-mi:“MI:0914”(association)0.570
KRTAP5-9SCARB1psi-mi:“MI:0915”(physical association)0.560
KRTAP10-9SCARB1psi-mi:“MI:0915”(physical association)0.560
SCARB1KRTAP10-9psi-mi:“MI:0915”(physical association)0.560
SCARB1CD81psi-mi:“MI:0915”(physical association)0.560
SCARB1CSNK1Dpsi-mi:“MI:0915”(physical association)0.560
JUNSCARB1psi-mi:“MI:0915”(physical association)0.560
APPSCARB1psi-mi:“MI:0915”(physical association)0.560
CD81C2orf72psi-mi:“MI:0914”(association)0.530
repAGPSpsi-mi:“MI:0914”(association)0.530
FBXO2TMEM131Lpsi-mi:“MI:0914”(association)0.530
TMEM30BKLRG2psi-mi:“MI:0914”(association)0.530
DEFA1MANBApsi-mi:“MI:0914”(association)0.530
CLGNNPC1psi-mi:“MI:0914”(association)0.530
SCGB1D4EGFRpsi-mi:“MI:0914”(association)0.530
VAMP5NBASpsi-mi:“MI:0914”(association)0.530

BioGRID (186): KRTAP5-9 (Two-hybrid), KRTAP10-9 (Two-hybrid), SCARB1 (Affinity Capture-MS), SCARB1 (Affinity Capture-MS), SCARB1 (Affinity Capture-MS), SCARB1 (Affinity Capture-MS), SCARB1 (Affinity Capture-MS), SCARB1 (Affinity Capture-MS), SCARB1 (Affinity Capture-MS), SCARB1 (Affinity Capture-MS), SCARB1 (Proximity Label-MS), SCARB1 (Proximity Label-MS), SCARB1 (Proximity Label-MS), SCARB1 (Affinity Capture-MS), SCARB1 (Affinity Capture-MS)

ESM2 similar proteins: A5A6J8, A5D7U4, O18824, O35114, O35409, P05026, P05027, P05028, P06583, P07340, P08251, P13638, P14094, P14231, P14415, P16671, P26201, P27615, P51168, P58421, P70110, P70627, P97943, Q07969, Q08857, Q14108, Q28030, Q2HZ96, Q4R4V5, Q4R5C3, Q5F362, Q5J583, Q5R8S8, Q60417, Q61009, Q6P9A2, Q708S3, Q708S7, Q7T2D4, Q8L8W0

Diamond homologs: O18824, O35114, P16671, P26201, P27615, P70110, P97943, Q07969, Q08857, Q14108, Q27367, Q60417, Q61009, Q8SQC1, Q8WTV0, Q11124, Q55FQ9, Q9BKJ9, Q9XYS8, E1JI63, C3U0S3, P86905, B2RFN2, Q7Q6R1, B7Z031

SIGNOR signaling

1 interactions.

AEffectBMechanism
SCARB1“up-regulates activity”SRCbinding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 105 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
Interferon gamma signaling712.4×2e-04
Downstream TCR signaling59.0×3e-03
Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell67.4×2e-03
MHC class II antigen presentation56.3×9e-03
Neutrophil degranulation113.6×3e-03

GO biological processes:

GO termPartnersFoldFDR
peptide antigen assembly with MHC class II protein complex556.6×1e-05
antigen processing and presentation of exogenous peptide antigen via MHC class II529.2×2e-04
positive regulation of T cell mediated cytotoxicity527.5×2e-04
positive regulation of immune response525.9×2e-04
positive regulation of T cell activation523.8×3e-04
ERAD pathway59.7×9e-03
adaptive immune response87.2×1e-03
immune response115.6×5e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic1
Likely pathogenic0
Uncertain significance83
Likely benign66
Benign36

Top pathogenic / likely-pathogenic (1)

Variant IDHGVSClassification
1334398NM_005505.5(SCARB1):c.727-2A>CPathogenic

SpliceAI

2682 predictions. Top by Δscore:

VariantEffectΔscore
12:124778585:CC:Cacceptor_gain1.0000
12:124778586:CC:Cacceptor_gain1.0000
12:124786355:A:ACdonor_gain1.0000
12:124786356:C:CCdonor_gain1.0000
12:124786356:CTTGG:Cdonor_gain1.0000
12:124786499:CCGCT:Cacceptor_gain1.0000
12:124786500:CGCT:Cacceptor_gain1.0000
12:124786500:CGCTC:Cacceptor_gain1.0000
12:124786502:CT:Cacceptor_gain1.0000
12:124787405:CCT:Cdonor_gain1.0000
12:124807759:A:ACdonor_gain1.0000
12:124807760:C:CCdonor_gain1.0000
12:124807760:CTGAA:Cdonor_gain1.0000
12:124811864:CCTCA:Cdonor_loss1.0000
12:124811865:CTCA:Cdonor_loss1.0000
12:124811866:TCACC:Tdonor_loss1.0000
12:124811867:CACC:Cdonor_loss1.0000
12:124811868:ACCT:Adonor_loss1.0000
12:124811869:C:Adonor_loss1.0000
12:124811869:CCTTG:Cdonor_gain1.0000
12:124811965:GCTA:Gacceptor_loss1.0000
12:124811966:C:CCacceptor_gain1.0000
12:124811967:T:Gacceptor_loss1.0000
12:124814197:CGTA:Cdonor_loss1.0000
12:124814200:ACCTC:Adonor_loss1.0000
12:124814201:CCT:Cdonor_gain1.0000
12:124814401:GCACC:Gacceptor_gain1.0000
12:124814402:CACC:Cacceptor_gain1.0000
12:124814402:CACCC:Cacceptor_gain1.0000
12:124814403:ACC:Aacceptor_gain1.0000

AlphaMissense

3384 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
12:124807810:G:CF320L0.999
12:124807810:G:TF320L0.999
12:124807812:A:GF320L0.999
12:124810174:C:GR281P0.999
12:124817666:C:AW56C0.999
12:124817666:C:GW56C0.999
12:124817668:A:GW56R0.999
12:124817668:A:TW56R0.999
12:124795224:G:CS391R0.998
12:124795224:G:TS391R0.998
12:124795226:T:GS391R0.998
12:124795261:C:TG379E0.998
12:124810249:C:TG256E0.998
12:124810278:C:AW246C0.998
12:124810278:C:GW246C0.998
12:124800225:A:GS343P0.997
12:124810249:C:AG256V0.997
12:124810280:A:GW246R0.997
12:124810280:A:TW246R0.997
12:124811926:C:AG224W0.997
12:124807871:C:GR300P0.996
12:124810232:A:GW262R0.996
12:124810232:A:TW262R0.996
12:124815065:A:GS112P0.996
12:124795261:C:AG379V0.995
12:124807811:A:CF320C0.995
12:124807811:A:GF320S0.995
12:124807847:A:CF308C0.995
12:124807867:G:CF301L0.995
12:124807867:G:TF301L0.995

dbSNP variants (sampled 300 via entrez): RS1000071346 (12:124776754 C>T), RS1000087143 (12:124820329 A>G), RS1000113702 (12:124844529 G>A,T), RS1000118237 (12:124820078 G>A), RS1000191070 (12:124793509 T>C,G), RS1000210253 (12:124835043 T>C), RS1000224412 (12:124838203 C>G), RS1000295721 (12:124845998 C>T), RS1000299400 (12:124838491 G>A), RS1000322657 (12:124798216 G>A,C), RS1000354923 (12:124812735 C>T), RS1000490707 (12:124827730 C>A,G), RS1000532925 (12:124856801 G>A,C), RS1000534197 (12:124786879 C>A), RS1000569502 (12:124780347 T>C)

Disease associations

OMIM: gene MIM:601040 | disease phenotypes: MIM:189800

GenCC curated gene-disease

Mondo (2): preeclampsia (MONDO:0005081), primary ovarian failure (MONDO:0005387)

Orphanet (2): Preeclampsia (Orphanet:275555), NON RARE IN EUROPE: Primary ovarian failure (Orphanet:619)

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

66 associations (top):

StudyTraitp-value
GCST000671_5Lipoprotein-associated phospholipase A2 activity and mass1.000000e-08
GCST000755_41HDL cholesterol3.000000e-14
GCST000907_1Renal cell carcinoma3.000000e-08
GCST001142_3Vitamin E levels8.000000e-09
GCST001727_2Lipoprotein-associated phospholipase A2 activity and mass6.000000e-14
GCST002223_51HDL cholesterol6.000000e-32
GCST002899_39HDL cholesterol2.000000e-18
GCST003445_1Response to cyclophosphamide in systemic lupus erythematosus with lupus nephritis6.000000e-07
GCST004232_9HDL cholesterol levels1.000000e-34
GCST004787_55Coronary artery disease (myocardial infarction, percutaneous transluminal coronary angioplasty, coronary artery bypass grafting, angina or chromic ischemic heart disease)4.000000e-09
GCST004963_7Lipoprotein phospholipase A2 activity in cardiovascular disease7.000000e-09
GCST005194_45Coronary artery disease2.000000e-13
GCST005194_46Coronary artery disease2.000000e-08
GCST005195_128Coronary artery disease2.000000e-18
GCST005196_72Coronary artery disease3.000000e-20
GCST005980_2Total bilirubin levels4.000000e-11
GCST006005_22High density lipoprotein cholesterol levels1.000000e-32
GCST006034_24Total cholesterol levels6.000000e-09
GCST006481_19Lung function (FEV1)5.000000e-08
GCST006611_100HDL cholesterol8.000000e-43
GCST006613_116Triglycerides3.000000e-14
GCST007827_1Alzheimer’s disease or HDL levels (pleiotropy)4.000000e-09
GCST007931_66Medication use (HMG CoA reductase inhibitors)2.000000e-08
GCST008035_78High density lipoprotein cholesterol levels4.000000e-09
GCST008070_118HDL cholesterol levels3.000000e-20
GCST008070_51HDL cholesterol levels2.000000e-24
GCST008075_148HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)7.000000e-44
GCST008075_208HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)1.000000e-24
GCST008075_33HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)7.000000e-19
GCST008084_153HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)8.000000e-49

EFO canonical traits (17, from GWAS)

EFO IDTrait name
EFO:0004746lipoprotein-associated phospholipase A(2) measurement
EFO:0004612high density lipoprotein cholesterol measurement
EFO:0004570bilirubin measurement
EFO:0004574total cholesterol measurement
EFO:0004314forced expiratory volume
EFO:0004530triglyceride measurement
EFO:0009932HMG CoA reductase inhibitor use measurement
EFO:0004329alcohol drinking
EFO:0004611low density lipoprotein cholesterol measurement
EFO:0004614apolipoprotein A 1 measurement
EFO:0004615apolipoprotein B measurement
EFO:0004527mean corpuscular hemoglobin
EFO:0005091monocyte count
EFO:0007989monocyte percentage of leukocytes
EFO:0007874gut microbiome measurement
EFO:0007788BMI-adjusted waist-hip ratio
EFO:0008039BMI-adjusted hip circumference

MeSH disease descriptors (2)

DescriptorNameTree numbers
D011225Pre-EclampsiaC12.050.703.395.249
D016649Primary Ovarian InsufficiencyC12.050.351.500.056.630.750; C12.100.250.056.630.750; C19.391.630.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1914272 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,146 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1208829ITX-5061 FREE BASE298
CHEMBL275707RIMCAZOLE21,048

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

PharmGKB clinical annotations

3 annotations.

VariantTypeLevelDrugsPhenotypes
rs10846744Efficacy3peginterferon alfa-2a;ribavirinChronic hepatitis C virus infection
rs4238001Efficacy3fenofibrateHypertriglyceridemia
rs5888Efficacy3atorvastatinHypercholesterolemia

PharmGKB variants

4 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs5888SCARB132.751atorvastatin
rs4238001SCARB133.501fenofibrate
rs10846744SCARB132.501peginterferon alfa-2a;ribavirin
rs3782287SCARB10.000

ChEMBL bioactivities

54 potent at pChembl≥5 of 54 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.82IC501.5nMCHEMBL2179510
8.82IC501.5nMCHEMBL2179485
8.82IC501.5nMCHEMBL2179515
8.82IC501.5nMCHEMBL2179514
8.82IC501.5nMCHEMBL2179511
8.82IC501.5nMCHEMBL2179509
8.82IC501.5nMCHEMBL2179508
8.82IC501.5nMCHEMBL2179507
8.82IC501.5nMCHEMBL2179504
8.82IC501.5nMCHEMBL2179502
8.82IC501.5nMCHEMBL2179501
8.82IC501.5nMCHEMBL2179500
8.82IC501.5nMCHEMBL2179499
8.82IC501.5nMCHEMBL2179493
8.82IC501.5nMCHEMBL1914885
8.30IC505nMCHEMBL2179106
8.30IC505nMCHEMBL2179512
8.30IC505nMCHEMBL2179497
8.00IC5010nMCHEMBL2179488
7.82IC5015nMCHEMBL2179487
7.82IC5015nMCHEMBL2179486
7.82IC5015nMCHEMBL2179513
7.82IC5015nMCHEMBL2179506
7.82IC5015nMCHEMBL2179498
7.82IC5015nMCHEMBL2177128
7.82IC5015nMCHEMBL2179494
7.52IC5030nMCHEMBL2179490
7.40IC5039.81nMCHEMBL3785336
7.30IC5050nMCHEMBL2179505
7.30IC5050nMCHEMBL2179503
7.30IC5050nMCHEMBL2179496
7.30IC5050nMCHEMBL2179495
7.30IC5050nMCHEMBL2179492
7.30IC5050nMCHEMBL2179489
7.30IC5050.12nMCHEMBL3786653
7.30IC5050.12nMCHEMBL3785828
7.30IC5050.12nMCHEMBL3785750
7.30IC5050.12nMCHEMBL3787085
7.10IC5079.43nMCHEMBL3785219
7.00IC50100nMITX-5061 FREE BASE
6.80IC50158.5nMCHEMBL3786659
6.80IC50158.5nMCHEMBL3786730
6.70IC50199.5nMCHEMBL3785530
6.64IC50230nMCHEMBL1914861
6.30IC50500nMCHEMBL2179491
6.30IC50501.2nMCHEMBL3787449
6.22IC50600nMCHEMBL1914862
6.20IC50630nMCHEMBL1914863
6.00IC501000nMCHEMBL3786485
6.00IC501000nMCHEMBL3786591

PubChem BioAssay actives

54 with measured affinity, of 62 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.

CompoundAssayTypeValueUnit
methyl 9-[3-(4,6-dimethylpyrimidin-2-yl)oxypropyl]-5,6,7,8-tetrahydrocarbazole-3-carboxylate704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
2-[9-[3-(4,6-dimethylpyrimidin-2-yl)oxypropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-1,3-oxazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-6-(tetrazol-1-yl)-1,2,3,4-tetrahydrocarbazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
5-[9-[3-(3,5-difluorophenoxy)propyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
5-[9-[3-(3,4-difluorophenoxy)propyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
5-[9-[3-(3,5-difluorophenyl)sulfanylpropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704911: Inhibition of human SRB1-mediated Hepatitis C virus genotype 1a entry into human HuH7.5 cells by immunoblottingic500.0015uM
5-[9-[3-(3,4-difluorophenyl)sulfanylpropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
5-[9-[3-(6-fluoro-1H-benzimidazol-2-yl)propyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
5-[9-[3-(3,5-difluorophenoxy)-2-fluoropropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)-2,3-dihydro-1H-carbazol-4-one704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
5-[9-[3-(4,6-dimethylpyrimidin-2-yl)oxypropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
5-[9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
3-methyl-5-[9-[3-[4-methyl-6-(trifluoromethyl)pyrimidin-2-yl]oxypropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
N,N-dimethyl-3-[6-(3-methyl-1,2,4-oxadiazol-5-yl)-1,2,3,4-tetrahydrocarbazol-9-yl]propane-1-sulfonamide704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-6-nitro-1,2,3,4-tetrahydrocarbazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0015uM
5-[9-[3-(3,5-difluorophenyl)sulfonylpropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0050uM
9-[3-(3,5-difluorophenyl)sulfanylpropyl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)-2,3-dihydro-1H-carbazol-4-one704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0050uM
3-[9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-5-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0050uM
4,6-dimethoxy-N-[3-(6-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-9-yl)propyl]pyrimidin-2-amine704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0100uM
9-[3-[(4,6-dimethoxypyrimidin-2-yl)amino]propyl]-5,6,7,8-tetrahydrocarbazole-3-carbonitrile704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0150uM
9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-6-(4-propyltriazol-1-yl)-1,2,3,4-tetrahydrocarbazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0150uM
5-[9-[3-(3,5-difluorophenyl)sulfinylpropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0150uM
5-[9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-6,6-difluoro-7,8-dihydro-5H-carbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0150uM
5-[9-[3-(3,5-difluorophenyl)sulfanylpropyl]-6,6-difluoro-7,8-dihydro-5H-carbazol-3-yl]-3-methyl-1,2,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0150uM
9-[3-(4,6-dimethylpyrimidin-2-yl)oxypropyl]-5,6,7,8-tetrahydrocarbazole-3-carbonitrile704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0150uM
2-[9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-5-methyl-1,3,4-oxadiazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0150uM
9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-6-methylsulfonyl-1,2,3,4-tetrahydrocarbazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0300uM
N-[3-[3-[bis(2-hydroxyethyl)amino]propylsulfonylamino]-5-tert-butyl-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.0398uM
3-(6-cyano-1,2,3,4-tetrahydrocarbazol-9-yl)-N,N-dimethylpropane-1-sulfonamide704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0500uM
9-[3-(4,6-dimethylpyrimidin-2-yl)oxypropyl]-6-methylsulfonyl-1,2,3,4-tetrahydrocarbazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0500uM
2-[9-[3-(4,6-dimethylpyrimidin-2-yl)oxypropyl]-5,6,7,8-tetrahydrocarbazol-3-yl]-4,5-dihydro-1,3-oxazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0500uM
9-[3-(4,6-diethylpyrimidin-2-yl)oxypropyl]-6-[4-(fluoromethyl)triazol-1-yl]-1,2,3,4-tetrahydrocarbazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0500uM
9-[3-(1H-benzimidazol-2-yl)propyl]-6-methylsulfonyl-1,2,3,4-tetrahydrocarbazole704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0500uM
9-[3-(1H-benzimidazol-2-yl)propyl]-5,6,7,8-tetrahydrocarbazole-3-carbonitrile704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.0500uM
N-[5-tert-butyl-3-[3-[[1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl]amino]propylsulfonylamino]-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.0501uM
N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-[4-(4-morpholin-4-ylbutoxy)naphthalen-1-yl]-2-oxoacetamide1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.0501uM
2-[4-[2-[(2-aminoacetyl)amino]ethoxy]naphthalen-1-yl]-N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-oxoacetamide1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.0501uM
N-[5-tert-butyl-2-methoxy-3-(propylsulfonylamino)phenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.0501uM
2-[4-[2-[bis(2-hydroxyethyl)amino]ethoxy]naphthalen-1-yl]-N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-oxoacetamide1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.0794uM
N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.1000uM
3-[[5-tert-butyl-2-methoxy-3-[[2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetyl]amino]phenyl]sulfamoyl]propyl-triethylazanium;2,2,2-trifluoroacetate1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.1585uM
N-[3-(4-aza-1-azoniabicyclo[2.2.2]octan-1-ylmethylsulfonylamino)-5-tert-butyl-2-methoxyphenyl]-2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide chloride1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.1585uM
2-[[5-tert-butyl-2-methoxy-3-[[2-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetyl]amino]phenyl]sulfamoyl]acetic acid1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.1995uM
methyl 9-[3-[(3R,5S)-3,5-dimethylpiperazin-1-yl]propyl]carbazole-3-carboxylate630155: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human 293T cells by immunoblottingic500.2300uM
N,N-dimethyl-3-(6-methylsulfonyl-1,2,3,4-tetrahydrocarbazol-9-yl)propane-1-sulfonamide704937: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human HuH7.5 cells by luciferase reporter gene assayic500.5000uM
2-[4-[2-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyanilino]-2-oxoacetyl]naphthalen-1-yl]oxyethyl-trimethylazanium;2,2,2-trifluoroacetate1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic500.5012uM
ethyl 9-[3-[(3R,5S)-3,5-dimethylpiperazin-1-yl]propyl]carbazole-3-carboxylate630155: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human 293T cells by immunoblottingic500.6000uM
propan-2-yl 9-[3-[(3S,5R)-3,5-dimethylpiperazin-1-yl]propyl]carbazole-3-carboxylate630155: Inhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human 293T cells by immunoblottingic500.6300uM
N-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyphenyl]-2-[4-[2-(4-methylmorpholin-4-ium-4-yl)ethoxy]naphthalen-1-yl]-2-oxoacetamide;2,2,2-trifluoroacetate1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic501.0000uM
3-[2-[4-[2-[5-tert-butyl-3-(methanesulfonamido)-2-methoxyanilino]-2-oxoacetyl]naphthalen-1-yl]oxyethylamino]-3-oxopropanoic acid1291805: Inhibition of human SR-B1 transiently expressed in human U2OS cells assessed as Dil-HDL uptake preincubated for 2 hrs followed by Dil-HDL addition measured after 2 hrs by FLIPR assayic501.0000uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Cyclosporineaffects cotreatment, decreases expression4
Resveratroldecreases expression, decreases reaction, affects cotreatment, increases expression3
Aspirinaffects expression, affects cotreatment, increases expression, decreases reaction, decreases activity (+2 more)3
Benzo(a)pyreneaffects methylation, decreases expression, increases methylation3
Estradioldecreases reaction, increases expression3
Valproic Acidaffects expression, decreases expression, increases expression, increases methylation3
Particulate Matterincreases expression, decreases expression, increases abundance3
bisphenol Aaffects expression, decreases methylation2
cobaltous chloridedecreases expression2
perfluorooctanoic aciddecreases expression2
entinostatincreases expression, affects cotreatment2
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamidedecreases expression, increases expression, affects cotreatment2
Rosiglitazoneaffects cotreatment, increases expression2
Air Pollutantsdecreases expression, increases abundance2
Chenodeoxycholic Acidincreases expression, affects cotreatment, decreases expression2
Cisplatindecreases expression, affects cotreatment, increases expression2
Deoxycholic Acidaffects cotreatment, decreases expression, increases expression2
Ethinyl Estradioldecreases expression, increases reaction, affects expression, affects splicing, affects cotreatment2
Hydrocortisoneaffects cotreatment, decreases expression, decreases reaction2
Niacinincreases reaction, decreases reaction, increases expression, increases export2
Nickeldecreases expression2
Tobacco Smoke Pollutiondecreases reaction, affects binding, increases reaction, affects localization, increases expression (+2 more)2
Tretinoindecreases expression2
Aflatoxin B1affects expression, decreases expression2
FR900359decreases phosphorylation1
dicrotophosincreases expression1
selenomethylselenocysteineincreases expression1
diphenyleneiodoniumdecreases expression, decreases reaction1
ascorbate-2-phosphateaffects binding, affects cotreatment, increases expression1
diethyl maleatedecreases expression1

ChEMBL screening assays

4 unique, capped per target: 4 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1918056BindingInhibition of human SRB1-mediated Hepatitis C virus genotype 2a entry into human 293T cells by immunoblottingDiscovery of highly potent small molecule Hepatitis C Virus entry inhibitors. — Bioorg Med Chem Lett

Cellosaurus cell lines

11 cell lines: 5 cancer cell line, 2 transformed cell line, 2 spontaneously immortalized cell line, 2 induced pluripotent stem cell

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_B7Z9Abcam Raji SCARB1 KOCancer cell lineMale
CVCL_B9W5Abcam HEK293T SCARB1 KOTransformed cell lineFemale
CVCL_C0A2Abcam THP-1 SCARB1 KOCancer cell lineMale
CVCL_C7BQAbcam PC-3 SCARB1 KOCancer cell lineMale
CVCL_E8TMCHO-SR-B1Spontaneously immortalized cell lineFemale
CVCL_E8TNCHO-CD81/SR-B1Spontaneously immortalized cell lineFemale
CVCL_E8TP293-SR-B1Transformed cell lineFemale
CVCL_EL59PENN159i-M14-4Induced pluripotent stem cellFemale
CVCL_EL62PENN162i-M14-11Induced pluripotent stem cellFemale
CVCL_TK10HAP1 SCARB1 (-) 1Cancer cell lineMale

Clinical trials (associated diseases)

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

TrialPhaseStatusTitle
NCT00117546PHASE4UNKNOWNCardiovascular and Autonomic Reactivity in Women With a History of Pre-eclampsia
NCT00567957PHASE4UNKNOWNRemifentanil for General Anesthesia in Preeclamptics
NCT01030627PHASE4COMPLETEDTreatment Approaches to Preeclampsia
NCT01352234PHASE4COMPLETEDComparison of Doses of Acetylsalicylic Acid in Women With Previous History of Preeclampsia
NCT01361425PHASE4UNKNOWNAnti-Hypertensive Treatment In Stable Pregnant Women With Severe Pre-Eclampsia (Metildopape)
NCT01729468PHASE4COMPLETEDPrevention of Pre-eclampsia and SGA by Low-Dose Aspirin in Nulliparous Women With Abnormal First-trimester Uterine Artery Dopplers
NCT01761916PHASE4COMPLETEDClonidine Versus Captopril for Treatment of Postpartum Very High Blood Pressure
NCT01912677PHASE4COMPLETEDOral Antihypertensive Regimens for Management of Hypertension in Pregnancy
NCT02025426PHASE4TERMINATEDPhenylephrine Versus Ephedrine in Pre-eclampsia
NCT02091401PHASE4COMPLETEDA Trial Comparing Treatment With the Springfusor Infusion Pump to the IV Magnesium Sulfate Regimen
NCT02163655PHASE4COMPLETEDDiuretics for Postpartum High Blood Pressure in Preeclampsia
NCT02338687PHASE4COMPLETEDLow Dose Calcium to Prevent Preeclampsia
NCT02396030PHASE4TERMINATEDDifferent Schemes of Magnesium Sulfate for Preeclampsia
NCT02531490PHASE4UNKNOWNEarly Vascular Adjustments During Hypertensive Pregnancy
NCT02699827PHASE4COMPLETEDAdding MgSO4 to Epidural Levobupivacaine in CS for Patients With Preeclampsia
NCT02835339PHASE4COMPLETEDMagnesium Sulfate in Obese Preeclamptics
NCT02891174PHASE4COMPLETEDThe Effect of Ibuprofen on Post-partum Blood Pressure in Women With Hypertensive Disorders of Pregnancy
NCT02911701PHASE4COMPLETEDEffect of Acetaminophen on Postpartum Blood Pressure Control in Preeclampsia With Severe Features
NCT03171480PHASE4COMPLETEDUse of Nitrous Oxide Donor for Labor Induction in Women With PreEclampsia
NCT03233880PHASE4UNKNOWNImpact of Antichlamydial Treatment on the Rate of Preeclampsia
NCT03237000PHASE4UNKNOWNEffect of Administering Intravenous Magnesium Sulfate on Fetal Cardiotocography and Neonatal Outcome in Preeclamptic Patients
NCT03506724PHASE4COMPLETEDResponse to Anti-hypertensives in Pregnant and Postpartum Patients
NCT03674606PHASE4COMPLETEDTrial of Early Screening Test for Pre-eclampsia and Growth Restriction
NCT03735433PHASE4TERMINATEDThe Effect of Two Aspirin Dosing Strategies for Obese Women at High Risk for Preeclampsia
NCT03824119PHASE4UNKNOWNPostpartum NSAIDS and Maternal Hypertension
NCT04051567PHASE4UNKNOWNLow-dose Aspirin for Prevention of Adverse Pregnancy Outcomes in Twin Pregnancies
NCT04077853PHASE4COMPLETEDProgesterone in Expectantly Managed Early-onset Preeclampsia
NCT04158830PHASE4WITHDRAWNAspirin (ASA) Therapy and Preeclampsia Prevention
NCT04424693PHASE4UNKNOWNComparing the Incidence of Preeclampsia Between Pregnant Women Receiving Tdap Vaccinations at Week 28 or at Week 36
NCT04631627PHASE4UNKNOWNEarly Prediction and Randomised Prevention of Preeclampsia With Low Dose Aspirin in Chinese Cohort
NCT04656665PHASE4UNKNOWNThe Effectiveness of Aspirin on Preventing Pre-eclampsia
NCT04797949PHASE4WITHDRAWNAdherence to Universal Aspirin Compared to Screening Indicated Aspirin for Prevention of Preeclampsia
NCT04908982PHASE4UNKNOWNAspirin for the Prevention of Preeclampsia in Women With Stage 1 Hypertension
NCT05221164PHASE4UNKNOWN162 mg of Aspirin for Prevention of Preeclampsia
NCT05294952PHASE4UNKNOWNco Ihibtory Receptor in Preeclampsia
NCT05514847PHASE4ACTIVE_NOT_RECRUITINGLow Dose Aspirin for Preterm Preeclampsia Preventionmg/day Dose in High-risk Patients
NCT05586373PHASE4COMPLETEDIbuprofen vs Dipyrone After C-section in Preeclampsia
NCT06069102PHASE4COMPLETEDOptimal Blood Pressure Treatment Thresholds Postpartum
NCT06107335PHASE4NOT_YET_RECRUITINGEffect of Albumin Versus Routine Care on Hemodynamic Response and Stability in Patients With Preeclampsia Guided by a Non-invasive Hemodynamic Monitoring System During Cesarean Delivery With Spinal Anesthesia
NCT06281665PHASE4RECRUITINGTreatment With Aspirin After Preeclampsia: TAP Trial