OSBP

Summary

OSBP (oxysterol binding protein, HGNC:8503) is a protein-coding gene on chromosome 11q12.1, encoding Oxysterol-binding protein 1 (P22059). Lipid transporter involved in lipid countertransport between the Golgi complex and membranes of the endoplasmic reticulum: specifically exchanges sterol (cholesterol) with phosphatidylinositol 4-phosphate (PI4P, 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol 4-phosphate)), del…. It is a selective cancer dependency (DepMap: 43.0% of cell lines).

Oxysterol binding protein is an intracellular protein that is believed to transport sterols from lysosomes to the nucleus where the sterol down-regulates the genes for the LDL receptor, HMG-CoA reductase, and HMG synthetase

Source: NCBI Gene 5007 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 66 total — 1 pathogenic
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 43.0% of screened cell lines
• MANE Select transcript: NM_002556

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8503
Approved symbol	OSBP
Name	oxysterol binding protein
Location	11q12.1
Locus type	gene with protein product
Status	Approved
Aliases	OSBP1
Ensembl gene	ENSG00000110048
Ensembl biotype	protein_coding
OMIM	167040
Entrez	5007

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 5 protein_coding, 1 nonsense_mediated_decay, 1 retained_intron

ENST00000263847, ENST00000525357, ENST00000528903, ENST00000937173, ENST00000937174, ENST00000942669, ENST00000942670

RefSeq mRNA: 1 — MANE Select: NM_002556 NM_002556

CCDS: CCDS7974

Canonical transcript exons

ENST00000263847 — 14 exons

Exon	Start	End
ENSE00000719163	59576805	59577025
ENSE00000719172	59593604	59593724
ENSE00000719176	59594010	59594255
ENSE00000719180	59600496	59600627
ENSE00000719184	59600819	59600873
ENSE00000719189	59601283	59601385
ENSE00000719194	59601640	59601838
ENSE00000719199	59608484	59608734
ENSE00000990742	59615303	59615774
ENSE00000990743	59610381	59610589
ENSE00001027972	59574398	59576719
ENSE00003471564	59581451	59581554
ENSE00003557250	59578149	59578330
ENSE00003623503	59580174	59580269

Expression profiles

Bgee: expression breadth ubiquitous, 298 present calls, max score 96.50.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 24.4383 / max 297.4962, expressed in 1816 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
119869	15.4665	1809
119868	8.3793	1772
119870	0.3537	135
119871	0.2387	82

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
type B pancreatic cell	CL:0000169	96.50	gold quality
jejunal mucosa	UBERON:0000399	95.38	gold quality
triceps brachii	UBERON:0001509	95.34	gold quality
corpus epididymis	UBERON:0004359	94.54	gold quality
right adrenal gland cortex	UBERON:0035827	94.53	gold quality
right adrenal gland	UBERON:0001233	94.50	gold quality
caput epididymis	UBERON:0004358	94.39	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	94.39	gold quality
biceps brachii	UBERON:0001507	94.10	gold quality
left adrenal gland	UBERON:0001234	94.09	gold quality
renal medulla	UBERON:0000362	94.00	gold quality
islet of Langerhans	UBERON:0000006	93.90	gold quality
jejunum	UBERON:0002115	93.71	gold quality
adrenal gland	UBERON:0002369	93.57	gold quality
adrenal cortex	UBERON:0001235	93.55	gold quality
left adrenal gland cortex	UBERON:0035825	93.48	gold quality
body of pancreas	UBERON:0001150	93.30	gold quality
cartilage tissue	UBERON:0002418	93.19	gold quality
pancreas	UBERON:0001264	93.15	gold quality
superficial temporal artery	UBERON:0001614	93.12	gold quality
skeletal muscle tissue	UBERON:0001134	93.07	gold quality
liver	UBERON:0002107	93.07	gold quality
deltoid	UBERON:0001476	92.95	gold quality
right lobe of liver	UBERON:0001114	92.91	gold quality
diaphragm	UBERON:0001103	92.89	gold quality
secondary oocyte	CL:0000655	92.81	gold quality
muscle of leg	UBERON:0001383	92.72	gold quality
muscle organ	UBERON:0001630	92.72	gold quality
skeletal muscle organ	UBERON:0014892	92.72	gold quality
gastrocnemius	UBERON:0001388	92.65	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	8.20
E-MTAB-6058	no	261.30

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

168 targeting OSBP, 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-5011-5P	100.00	83.46	5820
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-4476	100.00	68.18	2030
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-4510	100.00	66.60	2050
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-6129	100.00	66.46	2080
HSA-MIR-6130	100.00	66.69	2012
HSA-MIR-6133	100.00	66.48	2064
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-450A-1-3P	100.00	69.33	1837
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-3925-3P	100.00	69.95	1237
HSA-MIR-4534	99.99	66.58	1907
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-6077	99.99	68.04	2299
HSA-MIR-548N	99.98	71.94	4170
HSA-LET-7F-2-3P	99.98	70.98	2588
HSA-MIR-1185-1-3P	99.98	71.04	2593
HSA-MIR-1185-2-3P	99.98	71.04	2593

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 43.0% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 22)

• OSBP was found to function as a cholesterol-binding scaffolding protein coordinating the activity of two phosphatases to control the extracellular signal-regulated kinase (ERK) signaling pathway (PMID:15746430)
• Regulation of ceramide transport protein by OSBP, sterols, and vesicle-associated protein reveals a novel mechanism for integrating sterol regulatory signals with ceramide transport and phingomyelin synthesis in the Golgi apparatus. (PMID:16571669)
• OSBP is able to sense both membrane cholesterol and oxidized sterols and link this information to the ERK1/2 signaling pathway. (PMID:18165705)
• functional role of OSBP in the HCV maturation process. (PMID:19570870)
• Electrostatic interaction between oxysterol-binding protein and VAMP-associated protein A revealed by NMR and mutagenesis studies. (PMID:20178991)
• Results identify a novel substrate of protein kinase D at the Golgi, the oxysterol-binding protein OSBP. (PMID:20444975)
• This review summarizes recent evidence of sterol transfer activity by OSBP, suggesting seemingly disparate functions that could be the result of alterations in membrane sterol distribution or ancillary to this primary activity. (PMID:20545625)
• PKD negatively regulates HCV secretion/release by attenuating OSBP and CERT functions by phosphorylation inhibition. This study identifies the key role of the Golgi components in the HCV maturation process. (PMID:21285358)
• OSBP is required for efficient replication of intracellular S. Typhimurium. (PMID:21988961)
• Data indicate that phosphorylation on two serine-rich motifs, S381-S391 (site 1) and S192, S195, S200 (site 2), specifically controls oxysterol-binding protein (OSBP) activity at the endoplasmic reticulum (ER). (PMID:22875984)
• OSBP-mediated back transfer of phosphatidylinositol 4-phosphate might coordinate the transfer of other lipid species at the endoplasmic reticulum-Golgi interface. (PMID:24209621)
• These results suggest that poliovirus proteins modulate PI4KB activity and provide PI4P for recruitment of OSBP to accumulate unesterified cholesterol on virus-induced membrane structure for formation of a virus replication complex. (PMID:24527995)
• Our results identify OspB as a regulator of mTORC1 and mTORC1-dependent cell proliferation early during S. flexneri infection and establish a role for IQGAP1 in mTORC1 signaling (PMID:26473364)
• Data suggest that OSBP shifts the distribution of phosphatidylinositol 4-phosphate upon localization to endoplasmic reticulum-Golgi contact sites. (PMID:26601944)
• results demonstrate that Sac1 expression in either the ER or Golgi apparatus has a minimal impact on the PI-4P that regulates OSBP activity or recruitment to contact sites (PMID:28471037)
• Cholesterol transfer, PI4P consumption, and control of membrane lipid order by endogenous OSBP have been described. (PMID:28978670)
• the component proteins of the machinery, OSBP, VAP, SAC1, and PITPNB, are all essential host factors for AiV replication. Importantly, the machinery is directly recruited to the RNA replication sites through previously unknown interactions of VAP/OSBP/SAC1 with the AiV proteins and with ACBD3. (PMID:29367253)
• membrane cholesterol distribution contributes to insulin homeostasis at production, packaging, and export levels through the actions of OSBP and ABCs G1 and A1. (PMID:29540530)
• OSBP1 recruitment is required for SPI2-mediated alterations that promote vacuolar integrity of salmonellae. (PMID:31091452)
• The oxysterol binding protein (OSBP) is a storied protein in organelle biology. Its early roles include acting as a membrane contact site (MCS) tether as well as a lipid antiporter. (PMID:31103279)
• Molecular and cellular dissection of the oxysterol-binding protein cycle through a fluorescent inhibitor. (PMID:32075908)
• Oxysterol-Binding Protein: new insights into lipid transport functions and human diseases. (PMID:37455011)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	osbp	ENSDARG00000004634
mus_musculus	Osbp	ENSMUSG00000024687
rattus_norvegicus	Osbp	ENSRNOG00000021057
drosophila_melanogaster	CG3860	FBGN0034951
caenorhabditis_elegans		WBGENE00008832

Paralogs (11): OSBPL7 (ENSG00000006025), OSBPL5 (ENSG00000021762), OSBPL3 (ENSG00000070882), OSBPL6 (ENSG00000079156), OSBPL8 (ENSG00000091039), OSBPL9 (ENSG00000117859), OSBPL2 (ENSG00000130703), OSBPL1A (ENSG00000141447), OSBPL10 (ENSG00000144645), OSBPL11 (ENSG00000144909), OSBP2 (ENSG00000184792)

Protein

Protein identifiers

Oxysterol-binding protein 1 — P22059 (reviewed: P22059)

All UniProt accessions (2): P22059, H0YCV6

UniProt curated annotations — full annotation on UniProt →

Function. Lipid transporter involved in lipid countertransport between the Golgi complex and membranes of the endoplasmic reticulum: specifically exchanges sterol (cholesterol) with phosphatidylinositol 4-phosphate (PI4P, 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol 4-phosphate)), delivering sterol to the Golgi in exchange for PI4P, which is subsequently degraded by the SAC1/SACM1L phosphatase in the endoplasmic reticulum. Binds cholesterol and a range of oxysterols including 25-hydroxycholesterol. Cholesterol binding promotes the formation of a complex with PP2A and a tyrosine phosphatase which dephosphorylates ERK1/2, whereas 25-hydroxycholesterol causes its disassembly. Regulates cholesterol efflux by decreasing the stability of the relatively short lived ABCA1 protein (an important point of control for cholesterol efflux activity).

Subunit / interactions. Homodimer or homotrimer. Interacts (via FFAT motif) with VAPA. Interacts (via C-terminus) with RELCH (via the third HEAT repeat). Found in a complex composed of RELCH, OSBP1 and RAB11A.

Subcellular location. Cytoplasm. Cytosol. Perinuclear region. Golgi apparatus membrane. Endoplasmic reticulum membrane. Golgi apparatus. trans-Golgi network.

Tissue specificity. Widely expressed.

Domain organisation. The FFAT motif is required for interaction with VATA and proper localization of the protein. The PH and the Ala/Gly-rich domains control cholesterol binding without affecting 25-hydroxycholesterol binding. The second coiled-coil domain is required for interaction with the tyrosine phosphatase.

Similarity. Belongs to the OSBP family.

RefSeq proteins (1): NP_002547* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000648	Oxysterol-bd	Family
IPR001849	PH_domain	Domain
IPR011993	PH-like_dom_sf	Homologous_superfamily
IPR018494	Oxysterol-bd_CS	Conserved_site
IPR037239	OSBP_sf	Homologous_superfamily

Pfam: PF00169, PF01237

Catalyzed reactions (Rhea), 1 shown:

• a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol 4-phosphate)(out) + cholesterol(in) = a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol 4-phosphate)(in) + cholesterol(out) (RHEA:84179)

UniProt features (79 total): strand 19, modified residue 15, helix 15, binding site 8, turn 8, region of interest 3, compositionally biased region 2, mutagenesis site 2, coiled-coil region 2, initiator methionine 1, chain 1, domain 1, sequence variant 1, short sequence motif 1

Structure

Experimental structures (PDB)

2 structures.

PDB	Method	Resolution (Å)
7V62	X-RAY DIFFRACTION	3.25
2RR3	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P22059-F1	77.40	0.47

Functional residue map

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

Ligand- & substrate-binding residues (8): 117–122; 314; 314; 314; 314; 314; 493–496; 522–523

Post-translational modifications (15): 2, 190, 193, 198, 238, 240, 338, 345, 351, 377, 379, 382, 385, 386, 389

Mutagenesis-validated functional residues (2):

Position	Phenotype
108	impaired lipid exchange activity. induces a shift in subcellular location to the endoplasmic reticulum.
359–360	impaired lipid exchange activity. abolishes interaction with vapa.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-1660661	Sphingolipid de novo biosynthesis
R-HSA-192105	Synthesis of bile acids and bile salts

MSigDB gene sets: 285 (showing top): TGGTGCT_MIR29A_MIR29B_MIR29C, MYAATNNNNNNNGGC_UNKNOWN, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_VESICLE_ORGANIZATION, GOBP_INSULIN_SECRETION, GOBP_SPHINGOMYELIN_METABOLIC_PROCESS, GOBP_CELLULAR_RESPONSE_TO_CARBOHYDRATE_STIMULUS, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, GOBP_REGULATION_OF_HORMONE_LEVELS, TATTATA_MIR374, GOBP_HORMONE_TRANSPORT, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_ORGANELLE_ORGANIZATION, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS

GO Biological Process (10): sphingomyelin biosynthetic process (GO:0006686), bile acid biosynthetic process (GO:0006699), lipid transport (GO:0006869), phospholipid transport (GO:0015914), sterol transport (GO:0015918), intracellular cholesterol transport (GO:0032367), ceramide transport (GO:0035627), positive regulation of insulin secretion involved in cellular response to glucose stimulus (GO:0035774), positive regulation of secretory granule organization (GO:1904411), intermembrane lipid transfer (GO:0120009)

GO Molecular Function (8): oxysterol binding (GO:0008142), protein domain specific binding (GO:0019904), sterol binding (GO:0032934), phosphatidylinositol-4-phosphate binding (GO:0070273), lipid transfer activity (GO:0120013), sterol transfer activity (GO:0120015), protein binding (GO:0005515), lipid binding (GO:0008289)

GO Cellular Component (15): Golgi membrane (GO:0000139), nucleoplasm (GO:0005654), nucleolus (GO:0005730), cytoplasm (GO:0005737), endoplasmic reticulum membrane (GO:0005789), Golgi apparatus (GO:0005794), trans-Golgi network (GO:0005802), cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020), cell junction (GO:0030054), perinuclear region of cytoplasm (GO:0048471), perinuclear endoplasmic reticulum (GO:0097038), endoplasmic reticulum-trans-Golgi network membrane contact site (GO:0160258), endoplasmic reticulum (GO:0005783)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Sphingolipid metabolism	1
Bile acid and bile salt metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	7
lipid transport	4
cytoplasm	4
intracellular anatomical structure	2
sterol binding	2
binding	2
nuclear lumen	2
endomembrane system	2
intracellular membrane-bounded organelle	2
sphingomyelin metabolic process	1
phospholipid biosynthetic process	1
sphingolipid biosynthetic process	1
bile acid metabolic process	1
monocarboxylic acid biosynthetic process	1
transport	1
lipid localization	1
organophosphate ester transport	1
organic hydroxy compound transport	1
cholesterol transport	1
intracellular sterol transport	1
nitrogen compound transport	1
positive regulation of insulin secretion	1
insulin secretion involved in cellular response to glucose stimulus	1
regulation of insulin secretion involved in cellular response to glucose stimulus	1
positive regulation of organelle organization	1
secretory granule organization	1
regulation of secretory granule organization	1
membrane organization	1
protein binding	1
steroid binding	1
anion binding	1
phosphatidylinositol phosphate binding	1
transporter activity	1
lipid carrier activity	1
intermembrane lipid transfer	1
sterol transport	1
lipid transfer activity	1
Golgi apparatus	1
bounding membrane of organelle	1
intracellular membraneless organelle	1

Protein interactions and networks

STRING

1912 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
OSBP	VAPA	Q9P0L0	998
OSBP	ARF1	P10947	924
OSBP	PLEK2	Q9NYT0	910
OSBP	PLEK	P08567	908
OSBP	VAPB	O95292	822
OSBP	PI4KB	P78405	808
OSBP	ACBD3	Q9H3P7	750
OSBP	PITPNM1	O00562	727
OSBP	PI4KA	P42356	709
OSBP	SERPINA4	P29622	686
OSBP	STARD3	Q14849	673
OSBP	NPC1	O15118	669
OSBP	H1-8	Q8IZA3	659
OSBP	SCAP	Q12770	647
OSBP	ESYT1	Q9BSJ8	636

IntAct

105 interactions, top by confidence:

A	B	Type	Score
OSBP	VAPA	psi-mi:“MI:0915”(physical association)	0.890
OSBP	VAPA	psi-mi:“MI:2364”(proximity)	0.890
VAPB	FAM83G	psi-mi:“MI:0914”(association)	0.730
OSBP	FKBP6	psi-mi:“MI:0915”(physical association)	0.710
LRRC46	TFPT	psi-mi:“MI:0914”(association)	0.640
VAPA	FAM83G	psi-mi:“MI:0914”(association)	0.640
VAPA	PITPNM1	psi-mi:“MI:0914”(association)	0.640
BTN2A1	POTEF	psi-mi:“MI:0914”(association)	0.530
ZNRF4	UPK3BL1	psi-mi:“MI:0914”(association)	0.530
PCDHB16	UPK3BL1	psi-mi:“MI:0914”(association)	0.530
FKBP6	EEF2K	psi-mi:“MI:0914”(association)	0.530
LRRTM1	UPK3BL1	psi-mi:“MI:0914”(association)	0.530
CCDC107	PLD2	psi-mi:“MI:0914”(association)	0.530
sseL	OSBP	psi-mi:“MI:0915”(physical association)	0.520
OSBP	sseL	psi-mi:“MI:0915”(physical association)	0.520

BioGRID (208): OSBP (Affinity Capture-RNA), OSBP (Affinity Capture-MS), OSBP (Affinity Capture-MS), OSBP (Affinity Capture-MS), OSBP (Affinity Capture-MS), OSBP (Affinity Capture-MS), OSBP (Affinity Capture-MS), OSBP (Affinity Capture-MS), PPFIA1 (Co-fractionation), OSBP (Affinity Capture-MS), OSBP (Proximity Label-MS), OSBP (Proximity Label-MS), OSBP (Affinity Capture-MS), OSBP (Affinity Capture-MS), OSBP (Affinity Capture-MS)

ESM2 similar proteins: A2A8Z1, A8Y5H7, D2KC46, D3YXJ0, D3ZY60, E9PUQ8, F1M386, F1MS15, F1MSG6, F1PBJ0, O35889, O80866, O94512, O94830, P16258, P22059, P36583, P55196, Q0IJ05, Q15057, Q3B7Z2, Q3UYK3, Q5FVC7, Q5QNQ6, Q5R9W4, Q64398, Q6IVG4, Q6ZQK5, Q6ZT07, Q80W71, Q80Y98, Q86XP1, Q8BXR9, Q8CHG7, Q8CI95, Q8K4M9, Q8L751, Q91XL9, Q92503, Q93Y40

Diamond homologs: A0A223HDI2, A2BG43, B0BLT4, B0BNM9, B0YN54, D2KC46, D3ZY60, F1MS15, O14340, O22797, O95397, P16258, P22059, P35845, P68265, P68266, Q12451, Q3B7Z2, Q5M7Y0, Q5QNQ6, Q5R6M6, Q5U3N0, Q63ZQ3, Q6NRZ4, Q6NTN5, Q6NU44, Q6P3Q6, Q6VVX2, Q80W71, Q8C115, Q8IVE3, Q969R2, Q96JA3, Q9EQG9, Q9ERS4, Q9GKI7, Q9HB20, Q9JL62, Q9NZD2, Q9SAF0

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
PRKD1	down-regulates	OSBP	phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	39
Likely benign	4
Benign	3

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
599576	NM_002556.3(OSBP):c.1519C>T (p.Arg507Ter)	Pathogenic

SpliceAI

1851 predictions. Top by Δscore:

Variant	Effect	Δscore
11:59576720:C:CC	acceptor_gain	1.0000
11:59576799:CATTA:C	donor_loss	1.0000
11:59576800:ATTAC:A	donor_loss	1.0000
11:59576801:TTAC:T	donor_loss	1.0000
11:59576802:TACCA:T	donor_loss	1.0000
11:59576803:A:AC	donor_gain	1.0000
11:59576803:ACCA:A	donor_loss	1.0000
11:59576803:ACCAT:A	donor_gain	1.0000
11:59576804:C:CC	donor_gain	1.0000
11:59576804:CCAT:C	donor_gain	1.0000
11:59576804:CCATC:C	donor_gain	1.0000
11:59576807:T:TA	donor_gain	1.0000
11:59576828:T:TA	donor_gain	1.0000
11:59577022:CTTC:C	acceptor_gain	1.0000
11:59577023:TTC:T	acceptor_gain	1.0000
11:59577024:TC:T	acceptor_gain	1.0000
11:59577025:CC:C	acceptor_gain	1.0000
11:59577026:C:CC	acceptor_gain	1.0000
11:59577027:T:A	acceptor_loss	1.0000
11:59577032:G:C	acceptor_gain	1.0000
11:59577032:G:GC	acceptor_gain	1.0000
11:59580171:TACCT:T	donor_loss	1.0000
11:59580172:A:AT	donor_loss	1.0000
11:59580173:CCTTT:C	donor_gain	1.0000
11:59580265:CCAGA:C	acceptor_gain	1.0000
11:59580266:CAGA:C	acceptor_gain	1.0000
11:59580266:CAGAC:C	acceptor_gain	1.0000
11:59580267:AGA:A	acceptor_gain	1.0000
11:59580268:GA:G	acceptor_gain	1.0000
11:59580269:ACTGT:A	acceptor_loss	1.0000

AlphaMissense

5282 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:59576685:A:C	F772L	1.000
11:59576685:A:T	F772L	1.000
11:59576687:A:G	F772L	1.000
11:59576690:A:G	W771R	1.000
11:59576690:A:T	W771R	1.000
11:59576854:T:A	R744S	1.000
11:59576854:T:G	R744S	1.000
11:59576855:C:G	R744T	1.000
11:59576857:T:A	Q743H	1.000
11:59576857:T:G	Q743H	1.000
11:59576866:C:A	E740D	1.000
11:59576866:C:G	E740D	1.000
11:59576870:A:G	L739P	1.000
11:59576878:C:A	K736N	1.000
11:59576878:C:G	K736N	1.000
11:59576880:T:C	K736E	1.000
11:59576887:A:C	N733K	1.000
11:59576887:A:T	N733K	1.000
11:59576892:C:G	A732P	1.000
11:59576901:A:G	W729R	1.000
11:59576901:A:T	W729R	1.000
11:59576934:G:C	R718G	1.000
11:59576941:G:C	S715R	1.000
11:59576941:G:T	S715R	1.000
11:59576943:T:G	S715R	1.000
11:59576946:C:G	D714H	1.000
11:59576974:A:C	N704K	1.000
11:59576974:A:T	N704K	1.000
11:59578168:A:G	W681R	1.000
11:59578168:A:T	W681R	1.000

dbSNP variants (sampled 300 via entrez): RS1000135453 (11:59586500 T>C,G), RS1000154666 (11:59584453 G>A), RS1000227026 (11:59585906 T>A), RS1000233994 (11:59603016 A>C), RS1000300172 (11:59609785 C>A,T), RS1000375679 (11:59597273 G>A), RS1000424698 (11:59589786 C>T), RS1000426623 (11:59584751 T>C), RS1000433967 (11:59603362 G>A), RS1000552756 (11:59603009 A>C), RS1000589949 (11:59578201 C>A), RS1000833008 (11:59597853 G>A,C), RS1000859310 (11:59609621 T>A), RS1000864263 (11:59578557 G>A), RS1001008755 (11:59608164 C>T)

Disease associations

OMIM: gene MIM:167040 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523203 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 747,957 (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
CHEMBL112570	CHOLESTEROL	2	747,957

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

ChEMBL bioactivities

35 potent at pChembl≥5 of 35 total, top 35 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.22	Ki	6	nM	SCHWEINFURTHIN F
7.80	Ki	16	nM	CHEMBL375269
7.80	Ki	16	nM	CHEMBL5418635
7.66	Ki	22	nM	CHEMBL5405099
7.66	Kd	22	nM	CHEMBL169046
7.66	Kd	22	nM	SCHWEINFURTHIN G
7.62	Ki	24	nM	CHEMBL5429365
7.55	Ki	28	nM	CHEMBL5425718
7.51	Ki	31	nM	CHEMBL5397075
7.43	Ki	37	nM	CHEMBL5401329
7.41	Ki	39	nM	CEPHALOSTATIN 1
7.37	Ki	43	nM	CHEMBL5416867
7.34	Ki	46	nM	CHEMBL5414636
7.19	Ki	64	nM	CHEMBL5433096
7.17	Ki	68	nM	SCHWEINFURTHIN A
7.17	Ki	68	nM	CHEMBL353882
7.11	Ki	78	nM	CHEMBL4788348
7.10	Kd	80	nM	CHEMBL6166497
6.92	Ki	120	nM	CHEMBL5396576
6.92	Ki	120	nM	CHEMBL170154
6.92	Ki	119	nM	CHEMBL5394654
6.89	Ki	130	nM	CHEMBL173898
6.76	Kd	173	nM	CHOLESTEROL
6.59	Ki	254	nM	CHEMBL5417439
6.48	Ki	330	nM	CHEMBL171804
6.40	Ki	401	nM	SCHWEINFURTHIN H
6.40	Kd	401	nM	CHEMBL6169201
6.28	Ki	523	nM	CHEMBL5409120
6.22	Ki	600	nM	CHEMBL5424616
6.08	Ki	829	nM	CHEMBL5433829
5.97	Ki	1070	nM	CHEMBL5399392
5.89	Ki	1300	nM	CHEMBL5413783
5.52	Ki	3000	nM	MAPPAIN
5.49	Ki	3224	nM	CHEMBL5396667
5.43	Ki	3701	nM	CHEMBL5397623

PubChem BioAssay actives

37 with measured affinity, of 77 total; 37 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
(2S,3R,4aR,9aR)-7-[(E)-2-[3,5-dihydroxy-4-(3-methylbut-2-enyl)phenyl]ethenyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,3-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0010	uM
(2R,4aR,9aR)-7-[(E)-2-[3,5-dihydroxy-4-(3-methylbut-2-enyl)phenyl]ethenyl]-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,5-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0010	uM
(2R,4aR,9aR)-7-[2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethyl]-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,5-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0010	uM
(2R,4aR,9aR)-7-[(E)-2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethenyl]-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,5-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0010	uM
(2S,3R,4aR,9aR)-7-[(E)-2-[3,5-dihydroxy-4-(3-methylbut-2-enyl)phenyl]ethenyl]-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,3,5-triol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0010	uM
5-[(E)-2-[(7R,8aR,10aR)-7-hydroxy-4-methoxy-8,8,10a-trimethyl-6,7,8a,9-tetrahydro-5H-xanthen-2-yl]ethenyl]-2-(3-methylbut-2-enyl)benzene-1,3-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0060	uM
(2S,3R,4aR,9aR)-7-[(E)-2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethenyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,3-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0160	uM
[(2S,3R,4S,5R)-2-[(2S,3R,4S,5S)-3-acetyloxy-2-[[(3S,8R,9S,10R,13S,14S,16S,17S)-3,17-dihydroxy-10,13-dimethyl-17-[(2S)-6-methyl-3-oxoheptan-2-yl]-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-16-yl]oxy]-5-hydroxyoxan-4-yl]oxy-4,5-dihydroxyoxan-3-yl] 4-methoxybenzoate	1968548: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant	ki	0.0160	uM
(3S,8R,9S,10R,13S,14S,17S)-10,13,16,16-tetramethyl-3-(oxan-2-yloxy)-1,2,3,4,7,8,9,11,12,14,15,17-dodecahydrocyclopenta[a]phenanthren-17-ol	1968548: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant	ki	0.0220	uM
(3S,8S,9S,10R,13R,14S,17R)-17-[(2R)-6-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968550: Binding affinity to human OSBP	kd	0.0220	uM
(3S,8R,9S,10S,13R,14S,17R)-17-[(2R)-6-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	0.0240	uM
10440767	1968548: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant	ki	0.0280	uM
5-[(E)-2-[(7R,8aR,10aR)-7-hydroxy-8,8,10a-trimethyl-4-prop-2-enoxy-6,7,8a,9-tetrahydro-5H-xanthen-2-yl]ethenyl]-2-(3-methylbut-2-enyl)benzene-1,3-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0310	uM
5-[(E)-2-[(7aR,9R,11aR)-9-hydroxy-8,8,11a-trimethyl-2,7,7a,9,10,11-hexahydropyrano[3,2-c]xanthen-5-yl]ethenyl]-2-(3-methylbut-2-enyl)benzene-1,3-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0370	uM
10328411	1968548: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant	ki	0.0390	uM
5-[(E)-2-[(7R,8aR,10aR)-7-hydroxy-8,8,10a-trimethyl-4-prop-2-ynoxy-6,7,8a,9-tetrahydro-5H-xanthen-2-yl]ethenyl]-2-(3-methylbut-2-enyl)benzene-1,3-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0430	uM
(2R,4aR,9aR)-7-[2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthen-2-ol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0460	uM
(2R,4aR,9aR)-7-[(E)-2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethenyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthen-2-ol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.0640	uM
(3S,8S,9S,10R,13R,14S,17R)-17-[(2R,6R)-7-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	0.0680	uM
(2S,3R,4aR,9aR)-7-[(E)-2-[4-[(2E)-3,7-dimethylocta-2,6-dienyl]-3,5-dihydroxyphenyl]ethenyl]-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,3,5-triol	1968548: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant	ki	0.0680	uM
(3S,7S,8S,9S,10R,13R,14S,17R)-17-[(2R)-6-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene-3,7-diol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	0.0780	uM
(2R,4aR,9aR)-7-[(E)-2-[3,5-dihydroxy-4-(3-methylbut-2-enyl)phenyl]ethenyl]-1,1,4a-trimethyl-6-prop-2-enyl-3,4,9,9a-tetrahydro-2H-xanthene-2,5-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.1190	uM
(3S,8S,9S,10R,13R,14S,17R)-17-[(2R,5R)-5-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	0.1200	uM
(3S,8S,9S,10R,13R,14S,17R)-17-[(2R,6S)-7-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	0.1200	uM
(3S,8S,9S,10R,13S,14S,17S)-17-[(2S)-2-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	0.1300	uM
Cholesterol	1968550: Binding affinity to human OSBP	kd	0.1730	uM
(2R,4S,4aS,9aR)-7-[(E)-2-[3,5-dihydroxy-4-(3-methylbut-2-enyl)phenyl]ethenyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,4-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.2540	uM
(3S,8S,9S,10R,13R,14S,17R)-17-[(2R,5S)-5-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	0.3300	uM
(2S,3R,4aR,9aR)-7-[(E)-2-(3,5-dihydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethenyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthene-2,3-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.4010	uM
[(2R,4aR,9aR)-7-[(E)-2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethenyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthen-2-yl] formate	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.5230	uM
(3S,8S,9S,10R,13S,14S,17S)-17-[(2S)-2-hydroxyheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	0.6000	uM
[(2S,3R,4aR,9aR)-2-formyloxy-7-[(E)-2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethenyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthen-3-yl] formate	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	0.8290	uM
[(2R,4aR,9aR)-5-hydroxy-7-[(E)-2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethenyl]-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthen-2-yl] formate	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	1.0700	uM
(3S,8S,9S,10R,13S,14S,17S)-17-[(2S)-2-hydroxy-5-methylhexan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol	1968552: Displacement of [3H]-25-OHC from human OSBP overexpressed in HEK293T cell lysate assessed as inhibition constant by competitive binding assay	ki	1.3000	uM
5-[(E)-2-[3,5-dihydroxy-4-(3-methylbut-2-enyl)phenyl]ethenyl]-3-[(2E)-3,7-dimethylocta-2,6-dienyl]benzene-1,2-diol	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	3.0000	uM
[(2R,4aR,9aR)-5-hydroxy-7-[2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethyl]-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthen-2-yl] formate	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	3.2240	uM
[(2R,4aR,9aR)-7-[2-(5-hydroxy-2,2-dimethyl-3,4-dihydrochromen-7-yl)ethyl]-5-methoxy-1,1,4a-trimethyl-3,4,9,9a-tetrahydro-2H-xanthen-2-yl] formate	2019129: Inhibition of human C-terminal 6-His tagged OSBP ORD domain (401 to 807 residues) expressed in baculovirus-infected Sf9 cells assessed as reduction in DHE transfer from liposome (Le mimicking ER) to liposome (Lg mimicking golgi) with compound by FRET assay	ki	3.7010	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol F	increases expression	2
sodium arsenite	decreases expression, increases expression	2
Tobacco Smoke Pollution	affects expression, increases expression	2
Valproic Acid	decreases methylation, increases expression	2
Cyclosporine	increases expression	2
Palmitic Acid	decreases expression, decreases phosphorylation	2
Particulate Matter	increases reaction, affects cotreatment, decreases expression, increases abundance, affects expression	2
aristolochic acid I	increases expression	1
GSK-J4	increases expression	1
2,4,6-tribromophenol	decreases expression	1
propylparaben	increases expression	1
bisphenol A	decreases expression	1
potassium perchlorate	decreases expression	1
tetrabromobisphenol A	decreases expression	1
coumarin	increases phosphorylation	1
isobutyl alcohol	decreases expression, increases abundance, affects cotreatment	1
di-n-butylphosphoric acid	affects expression	1
perfluorooctane sulfonic acid	increases expression	1
CGP 52608	affects binding, increases reaction	1
K 7174	increases expression	1
oxidized-L-alpha-1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphorylcholine	affects expression, increases reaction	1
dimethylarsinous acid	increases expression	1
nutlin 3	affects cotreatment, increases secretion	1
ICG 001	decreases expression	1
bisphenol B	increases expression	1
(4-amino-1,4-dihydro-3-(2-pyridyl)-5-thioxo-1,2,4-triazole)copper(II)	increases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
Vehicle Emissions	affects expression, increases reaction	1
Benzene	increases expression	1

ChEMBL screening assays

30 unique, capped per target: 30 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4388957	Binding	Induction of OSBP localization in golgi apparatus of human HeLa cells assessed as increase in colocalization of 58K golgi protein at 5 nM incubated for 30 mins by immunofluorescence imaging method	Anticancer saponin OSW-1 is a novel class of selective Golgi stress inducer. — Bioorg Med Chem Lett

Clinical trials (associated diseases)

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