PSD

Summary

PSD (pleckstrin and Sec7 domain containing, HGNC:9507) is a protein-coding gene on chromosome 10q24.32, encoding PH and SEC7 domain-containing protein 1 (A5PKW4). Guanine nucleotide exchange factor for ARF6.

This gene encodes a Plekstrin homology and SEC7 domains-containing protein that functions as a guanine nucleotide exchange factor. The encoded protein regulates signal transduction by activating ADP-ribosylation factor 6. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 5662 — RefSeq curated summary.

At a glance

• GWAS associations: 6
• Clinical variants (ClinVar): 142 total
• Druggable target: yes
• MANE Select transcript: NM_002779

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:9507
Approved symbol	PSD
Name	pleckstrin and Sec7 domain containing
Location	10q24.32
Locus type	gene with protein product
Status	Approved
Aliases	KIAA2011, TYL, PSD1, EFA6A, EFA6
Ensembl gene	ENSG00000059915
Ensembl biotype	protein_coding
OMIM	602327
Entrez	5662

Gene structure

Transcript identifiers

Ensembl transcripts: 16 — 11 protein_coding, 5 protein_coding_CDS_not_defined

ENST00000020673, ENST00000406432, ENST00000461698, ENST00000472685, ENST00000473507, ENST00000479172, ENST00000488194, ENST00000492902, ENST00000611678, ENST00000864098, ENST00000864099, ENST00000864100, ENST00000864101, ENST00000864102, ENST00000933096, ENST00000933097

RefSeq mRNA: 3 — MANE Select: NM_002779 NM_001270965, NM_001270966, NM_002779

CCDS: CCDS31272, CCDS73187

Canonical transcript exons

ENST00000020673 — 17 exons

Exon	Start	End
ENSE00000722747	102403842	102403985
ENSE00000722749	102404583	102404727
ENSE00000722750	102404898	102405055
ENSE00000722753	102405346	102405536
ENSE00000722760	102411707	102411819
ENSE00000722762	102412381	102412575
ENSE00000811521	102402619	102403430
ENSE00000811524	102413769	102414197
ENSE00001313471	102416385	102417121
ENSE00001317785	102414863	102415229
ENSE00001415244	102418701	102418785
ENSE00002492513	102412147	102412227
ENSE00003273806	102416017	102416119
ENSE00003487570	102405183	102405253
ENSE00003523841	102411058	102411116
ENSE00003537392	102407223	102407266
ENSE00003545336	102410858	102410947

Expression profiles

Bgee: expression breadth ubiquitous, 188 present calls, max score 99.01.

FANTOM5 (CAGE): breadth broad, TPM avg 10.9893 / max 505.8670, expressed in 734 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
111157	5.8447	662
111162	2.0714	231
111165	1.6109	153
111164	0.8743	111
111161	0.3396	120
111167	0.1347	71
111158	0.1137	50

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right frontal lobe	UBERON:0002810	99.01	gold quality
cingulate cortex	UBERON:0003027	98.52	gold quality
anterior cingulate cortex	UBERON:0009835	98.50	gold quality
nucleus accumbens	UBERON:0001882	98.20	gold quality
muscle layer of sigmoid colon	UBERON:0035805	98.01	gold quality
amygdala	UBERON:0001876	97.88	gold quality
adenohypophysis	UBERON:0002196	97.20	gold quality
caudate nucleus	UBERON:0001873	97.17	gold quality
prefrontal cortex	UBERON:0000451	97.03	gold quality
Brodmann (1909) area 9	UBERON:0013540	96.67	gold quality
cortical plate	UBERON:0005343	96.63	gold quality
Brodmann (1909) area 10	UBERON:0013541	96.45	gold quality
putamen	UBERON:0001874	96.24	gold quality
right hemisphere of cerebellum	UBERON:0014890	95.56	gold quality
pituitary gland	UBERON:0000007	95.32	gold quality
cerebellar hemisphere	UBERON:0002245	95.01	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	94.88	gold quality
frontal cortex	UBERON:0001870	94.87	gold quality
neocortex	UBERON:0001950	94.87	gold quality
frontal lobe	UBERON:0016525	94.87	gold quality
lower esophagus muscularis layer	UBERON:0035833	94.86	gold quality
cerebellar cortex	UBERON:0002129	94.85	gold quality
frontal pole	UBERON:0002795	94.82	gold quality
lower esophagus	UBERON:0013473	94.77	gold quality
body of uterus	UBERON:0009853	94.18	gold quality
middle frontal gyrus	UBERON:0002702	94.11	gold quality
telencephalon	UBERON:0001893	93.54	gold quality
forebrain	UBERON:0001890	93.28	gold quality
cerebral cortex	UBERON:0000956	93.01	gold quality
Ammon’s horn	UBERON:0001954	92.77	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	3.01

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

66 targeting PSD, 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-4692	100.00	67.32	2066
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-4650-5P	99.98	64.69	999
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-454-3P	99.91	74.01	1925
HSA-MIR-130A-3P	99.90	73.31	1861
HSA-MIR-130B-3P	99.90	73.27	1850
HSA-MIR-301A-3P	99.90	73.15	1839
HSA-MIR-301B-3P	99.90	73.19	1836
HSA-MIR-3666	99.90	73.24	1833
HSA-MIR-4295	99.90	73.11	1838
HSA-MIR-106A-5P	99.90	73.94	2683
HSA-MIR-17-5P	99.89	73.83	2665
HSA-MIR-106B-5P	99.88	74.72	2795
HSA-MIR-20A-5P	99.88	74.76	2769
HSA-MIR-20B-5P	99.88	74.01	2621
HSA-MIR-519D-3P	99.88	73.97	2607
HSA-MIR-526B-3P	99.88	74.06	2587
HSA-MIR-93-5P	99.88	73.98	2606
HSA-MIR-4447	99.85	67.81	2900
HSA-MIR-548AZ-5P	99.83	69.94	3230
HSA-MIR-548T-5P	99.83	69.91	3220
HSA-MIR-6842-5P	99.80	67.54	1587
HSA-MIR-7110-5P	99.80	67.84	1712
HSA-MIR-548F-5P	99.78	71.02	3093
HSA-MIR-3150A-3P	99.76	64.44	1640
HSA-MIR-6763-5P	99.76	64.68	1767

Literature-anchored findings (GeneRIF, showing 8)

• Both levels of accumulation of F-actin and apoptosis were significantly decreased in specimens from UC patients with PSD methylation compared to those without PSD methylation. (PMID:22002136)
• Aberrant methylation of PSD occurs in UC-associated colorectal mucosa, enabling circumvention of Rac1 immune responses governing neutrophil chemotaxis and apoptosis, and plays a pivotal role in the mechanisms underlying UC-associated carcinogenesis. (PMID:22179719)
• EFA6 participates in activation of Arf6 around the cleavage furrow during cytokinesis. (PMID:23603394)
• EFA6 is regulated by a negative feedback loop, which is mediated by an allosteric interaction of Arf6-GTP with a domain of EFA6 and monitors the activation of Arf1 and Arf6 differentially (PMID:25114232)
• PSD expression might be a useful biomarker for epigenetic-based gastric cancer early diagnosis and may lead to the identification of new targets for pharmacological intervention. (PMID:25355626)
• Arf GTPases are likely to be locally activated by EFA6 and in turn targeted to the Flemming body to complete cytokinesis. (PMID:26330566)
• EFA6A recruits alpha-actinin 1 (ACTN1) through direct binding. (PMID:29246944)
• The C-terminal domain of EFA6A interacts directly with F-actin and assembles F-actin bundles. (PMID:31844082)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio		ENSDARG00000076702
danio_rerio	psda	ENSDARG00000078102
mus_musculus	Psd	ENSMUSG00000037126
rattus_norvegicus	Psd	ENSRNOG00000019435
drosophila_melanogaster	Efa6	FBGN0051158
caenorhabditis_elegans		WBGENE00013223

Paralogs (15): CYTH3 (ENSG00000008256), MON2 (ENSG00000061987), ARFGEF1 (ENSG00000066777), CYTH4 (ENSG00000100055), CYTH2 (ENSG00000105443), GBF1 (ENSG00000107862), CYTH1 (ENSG00000108669), IQSEC3 (ENSG00000120645), ARFGEF2 (ENSG00000124198), IQSEC2 (ENSG00000124313), PSD4 (ENSG00000125637), IQSEC1 (ENSG00000144711), PSD2 (ENSG00000146005), PSD3 (ENSG00000156011), FBXO8 (ENSG00000164117)

Protein

Protein identifiers

PH and SEC7 domain-containing protein 1 — A5PKW4 (reviewed: A5PKW4)

Alternative names: Exchange factor for ADP-ribosylation factor guanine nucleotide factor 6, Exchange factor for ARF6 A, Pleckstrin homology and SEC7 domain-containing protein 1

All UniProt accessions (2): A5PKW4, A0A1B0GUT6

UniProt curated annotations — full annotation on UniProt →

Function. Guanine nucleotide exchange factor for ARF6. Induces cytoskeletal remodeling.

Subunit / interactions. Interacts with ACTN1. Interacts (ARF6-bound form) with KCNK1; does not interact with KCNK1 in the absence of ARF6.

Subcellular location. Cell membrane. Cell projection. Ruffle membrane. Cleavage furrow.

Tissue specificity. Isoform 2 is expressed in the brain.

Similarity. Belongs to the PSD family.

Isoforms (2)

UniProt ID	Names	Canonical?
A5PKW4-1	1	yes
A5PKW4-2	2

RefSeq proteins (3): NP_001257894, NP_001257895, NP_002770* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000904	Sec7_dom	Domain
IPR001605	PH_dom-spectrin-type	Domain
IPR001849	PH_domain	Domain
IPR011993	PH-like_dom_sf	Homologous_superfamily
IPR023394	Sec7_C_sf	Homologous_superfamily
IPR035999	Sec7_dom_sf	Homologous_superfamily
IPR041681	PH_9	Domain

Pfam: PF01369, PF15410

UniProt features (25 total): compositionally biased region 7, region of interest 5, modified residue 3, sequence conflict 3, domain 2, mutagenesis site 2, chain 1, splice variant 1, coiled-coil region 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-A5PKW4-F1	56.76	0.21

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 (3): 126, 156, 720

Mutagenesis-validated functional residues (2):

Position	Phenotype
621	loss of gef activity, loss of arf6 localization to the cleavage furrow and, later in cytokinesis, to the midbody ring.
765–766	loss of localization to the plasma membrane during interphase and to the cleavage furrow during cytokinesis. no effect o

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 225 (showing top): TGCGCANK_UNKNOWN, TGCACTT_MIR519C_MIR519B_MIR519A, PEREZ_TP63_TARGETS, LFA1_Q6, GCANCTGNY_MYOD_Q6, GOBP_REGULATION_OF_SMALL_GTPASE_MEDIATED_SIGNAL_TRANSDUCTION, HSIAO_HOUSEKEEPING_GENES, GOBP_NEUROGENESIS, GOBP_VESICLE_MEDIATED_TRANSPORT, GOCC_RUFFLE, GGGTGGRR_PAX4_03, CAGCTG_AP4_Q5, MORF_RAD51L3, EFC_Q6, MODULE_66

GO Biological Process (3): signal transduction (GO:0007165), neuron projection development (GO:0031175), regulation of ARF protein signal transduction (GO:0032012)

GO Molecular Function (3): guanyl-nucleotide exchange factor activity (GO:0005085), phospholipid binding (GO:0005543), protein binding (GO:0005515)

GO Cellular Component (8): cleavage furrow (GO:0032154), ruffle membrane (GO:0032587), dendritic spine (GO:0043197), postsynaptic density, intracellular component (GO:0099092), plasma membrane (GO:0005886), postsynaptic density (GO:0014069), membrane (GO:0016020), cell projection (GO:0042995)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	2
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
neuron development	1
plasma membrane bounded cell projection organization	1
ARF protein signal transduction	1
regulation of small GTPase mediated signal transduction	1
GTP binding	1
GDP binding	1
GTPase regulator activity	1
lipid binding	1
binding	1
cell division site	1
plasma membrane region	1
ruffle	1
cell projection membrane	1
leading edge membrane	1
dendrite	1
neuron spine	1
postsynapse	1
postsynaptic density	1
postsynaptic specialization, intracellular component	1
membrane	1
cell periphery	1
asymmetric synapse	1
postsynaptic specialization	1

Protein interactions and networks

STRING

1048 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PSD	ARF6	P26438	824
PSD	PISD	Q9UG56	602
PSD	ARF1	P10947	593
PSD	ACAP1	Q15027	588
PSD	CHST15	Q7LFX5	582
PSD	CCNF	P41002	544
PSD	SNX1	Q13596	535
PSD	RABIF	P47224	527
PSD	GNA12	Q03113	477
PSD	ARF5	P26437	476
PSD	M0QZ92	M0QZ92	460
PSD	KCNJ5	P48544	453
PSD	GGA3	Q9NZ52	451
PSD	PLEK2	Q9NYT0	448
PSD	PLEK	P08567	447

IntAct

18 interactions, top by confidence:

A	B	Type	Score
Usp9x	PSD	psi-mi:“MI:0407”(direct interaction)	0.570
Usp9x	PSD	psi-mi:“MI:0915”(physical association)	0.570
PSD	Usp9x	psi-mi:“MI:0403”(colocalization)	0.570
PSD	Psmd4	psi-mi:“MI:0915”(physical association)	0.400
Eps15	PSD	psi-mi:“MI:0915”(physical association)	0.400
PSD	UBC	psi-mi:“MI:0915”(physical association)	0.400
PSD		psi-mi:“MI:0403”(colocalization)	0.270
TJP1	PSD	psi-mi:“MI:0403”(colocalization)	0.270
PSD	ARF6	psi-mi:“MI:0403”(colocalization)	0.270
HUS1	PSD	psi-mi:“MI:0915”(physical association)	0.000
HEXD	PSD	psi-mi:“MI:0915”(physical association)	0.000
PSD	GLRA2	psi-mi:“MI:0915”(physical association)	0.000
GMFG	PSD	psi-mi:“MI:0915”(physical association)	0.000
PSD	GNB5	psi-mi:“MI:0915”(physical association)	0.000
PSD	RAB40C	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (6): PSD (Affinity Capture-Western), PSD (Two-hybrid), PSD (Affinity Capture-MS), PSD (Positive Genetic), RAPGEFL1 (Cross-Linking-MS (XL-MS)), GNAQ (Affinity Capture-Western)

ESM2 similar proteins: A1L1I3, A5PKW4, O08919, O70405, O75385, O75420, O75553, P16554, P42128, P49757, P53814, P85037, P97318, P98081, Q04637, Q2LC84, Q3UCQ1, Q4KMP7, Q5DTT2, Q5I1X5, Q5RBR0, Q5VZ18, Q69ZH9, Q69ZI1, Q7TN02, Q7Z6J0, Q80VC9, Q80XI3, Q80Z38, Q86V15, Q8BGT6, Q8BHL3, Q8BSD5, Q8C120, Q8CI12, Q8IY33, Q8K4J6, Q8N3F8, Q8TEH3, Q8TEJ3

Diamond homologs: A0A0G2JUG7, A2A5R2, A5PKW4, D4A631, E1JIT7, F1MUS9, F4IXW2, F4JN05, F4JSZ5, F4K2K3, G3X9K3, G5EET6, O08967, O13690, O13817, O43739, O46382, P11075, P34512, P39993, P47102, P63034, P63035, P97694, P97696, Q10491, Q15438, Q2KI41, Q2PFD7, Q3TES0, Q42510, Q54KA7, Q5DTT2, Q5DU25, Q5E9G6, Q5JU85, Q6DFZ1, Q6DN90, Q6P1I6, Q76M68

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	111
Likely benign	14
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

3301 predictions. Top by Δscore:

Variant	Effect	Δscore
10:102403836:GCTCA:G	donor_loss	1.0000
10:102403837:CTCA:C	donor_loss	1.0000
10:102403838:TCACC:T	donor_loss	1.0000
10:102403839:CACCT:C	donor_loss	1.0000
10:102403840:A:AC	donor_gain	1.0000
10:102403841:C:A	donor_loss	1.0000
10:102403841:C:CA	donor_gain	1.0000
10:102403841:CCT:C	donor_gain	1.0000
10:102403861:T:TA	donor_gain	1.0000
10:102403983:CTC:C	acceptor_gain	1.0000
10:102403985:CCT:C	acceptor_loss	1.0000
10:102403986:C:A	acceptor_loss	1.0000
10:102403986:C:CC	acceptor_gain	1.0000
10:102403987:T:C	acceptor_loss	1.0000
10:102403990:C:CT	acceptor_gain	1.0000
10:102403991:G:T	acceptor_gain	1.0000
10:102403994:C:CT	acceptor_gain	1.0000
10:102403994:C:T	acceptor_gain	1.0000
10:102403995:A:T	acceptor_gain	1.0000
10:102404896:A:AC	donor_gain	1.0000
10:102404897:C:CG	donor_gain	1.0000
10:102404897:CGG:C	donor_gain	1.0000
10:102404897:CGGG:C	donor_gain	1.0000
10:102404897:CGGGG:C	donor_gain	1.0000
10:102405180:CACCT:C	donor_loss	1.0000
10:102405181:ACCT:A	donor_loss	1.0000
10:102405182:C:CA	donor_loss	1.0000
10:102405182:CCTT:C	donor_gain	1.0000
10:102405249:AGGTG:A	acceptor_gain	1.0000
10:102405250:GGTG:G	acceptor_gain	1.0000

AlphaMissense

6560 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
10:102404705:A:G	W860R	1.000
10:102404705:A:T	W860R	1.000
10:102404937:A:G	L839P	1.000
10:102405231:C:A	W783C	1.000
10:102405231:C:G	W783C	1.000
10:102405233:A:G	W783R	1.000
10:102405233:A:T	W783R	1.000
10:102405374:C:A	K766N	1.000
10:102405374:C:G	K766N	1.000
10:102407228:C:A	W710C	1.000
10:102407228:C:G	W710C	1.000
10:102407230:A:G	W710R	1.000
10:102407230:A:T	W710R	1.000
10:102410862:A:T	L696H	1.000
10:102410904:A:G	L682P	1.000
10:102410915:G:C	F678L	1.000
10:102410915:G:T	F678L	1.000
10:102410916:A:C	F678C	1.000
10:102410916:A:G	F678S	1.000
10:102410917:A:G	F678L	1.000
10:102410930:C:A	M673I	1.000
10:102410930:C:G	M673I	1.000
10:102410930:C:T	M673I	1.000
10:102410931:A:G	M673T	1.000
10:102411068:A:G	L664P	1.000
10:102411076:G:C	N661K	1.000
10:102411076:G:T	N661K	1.000
10:102411077:T:A	N661I	1.000
10:102411080:A:G	L660P	1.000
10:102411080:A:T	L660H	1.000

dbSNP variants (sampled 300 via entrez): RS1000325831 (10:102418414 T>C), RS1000477318 (10:102409480 G>C), RS1000621959 (10:102403767 C>T), RS1000635499 (10:102405228 C>A,T), RS1000886726 (10:102411808 T>A,C), RS1001114558 (10:102409248 CGCGGCG>C,CGCG,CGCGGCGGCG,CGCGGCGGCGGCG,CGCGGCGGCGGCGGCG), RS1001470627 (10:102410194 C>G), RS1001504637 (10:102403740 A>T), RS1001526280 (10:102405710 G>A), RS1001620539 (10:102403919 C>A,T), RS1001857451 (10:102410517 C>A), RS1002159288 (10:102421576 G>A,T), RS1002206188 (10:102421920 C>T), RS1002265992 (10:102415442 G>A), RS1002271349 (10:102404158 C>A)

Disease associations

OMIM: gene MIM:602327 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

6 associations (top):

Study	Trait	p-value
GCST001942_1	Prostate cancer	5.000000e-10
GCST005956_50	Waist-to-hip ratio adjusted for BMI	8.000000e-06
GCST005958_15	Waist-to-hip ratio adjusted for BMI (age >50)	4.000000e-06
GCST005962_36	Waist-to-hip ratio adjusted for BMI x sex x age interaction (4df test)	6.000000e-07
GCST010002_298	Refractive error	3.000000e-22
GCST010243_90	Apolipoprotein B levels	2.000000e-10

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0007788	BMI-adjusted waist-hip ratio
EFO:0008007	age at assessment
EFO:0008343	sex interaction measurement
EFO:0004615	apolipoprotein B measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523105 (SINGLE PROTEIN)

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1056890	NFKB2, PSD		0.00	0

ChEMBL bioactivities

128 potent at pChembl≥5 of 155 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.60	IC50	250	nM	CHEMBL4574541
6.48	IC50	330	nM	CHEMBL4560033
6.34	IC50	460	nM	CHEMBL4574204
6.30	IC50	500	nM	CHEMBL4525424
6.28	IC50	520	nM	CHEMBL4574204
6.25	IC50	560	nM	CHEMBL4540870
6.24	IC50	580	nM	CHEMBL4585299
6.18	IC50	660	nM	CHEMBL4534219
6.18	IC50	660	nM	CHEMBL4555543
6.17	IC50	670	nM	CHEMBL4540598
6.08	IC50	840	nM	CHEMBL4559227
6.06	IC50	880	nM	CHEMBL4531207
6.02	IC50	960	nM	CHEMBL4546661
6.02	IC50	960	nM	CHEMBL4591591
6.01	IC50	980	nM	CHEMBL4574371
6.00	IC50	1000	nM	CHEMBL4535892
5.96	IC50	1100	nM	CHEMBL4574955
5.96	IC50	1100	nM	CHEMBL4545638
5.96	IC50	1100	nM	CHEMBL4538242
5.96	IC50	1100	nM	CHEMBL4544503
5.96	IC50	1100	nM	CHEMBL4562282
5.96	IC50	1100	nM	CHEMBL4544792
5.96	IC50	1100	nM	CHEMBL4551164
5.96	IC50	1100	nM	CHEMBL4534219
5.96	IC50	1100	nM	CHEMBL593310
5.92	IC50	1200	nM	CHEMBL4538917
5.92	IC50	1200	nM	CHEMBL4522994
5.92	IC50	1200	nM	CHEMBL4571172
5.92	IC50	1200	nM	CHEMBL4522152
5.89	IC50	1300	nM	CHEMBL4570092
5.85	IC50	1400	nM	CHEMBL4537606
5.85	IC50	1400	nM	CHEMBL4584659
5.85	IC50	1400	nM	CHEMBL4553138
5.85	IC50	1400	nM	CHEMBL4570092
5.85	IC50	1400	nM	CHEMBL3716578
5.85	IC50	1400	nM	CHEMBL4584003
5.82	IC50	1500	nM	CHEMBL3716200
5.82	IC50	1500	nM	CHEMBL4579326
5.82	IC50	1500	nM	CHEMBL4553356
5.82	IC50	1500	nM	CHEMBL4528352
5.82	IC50	1500	nM	CHEMBL4564205
5.80	IC50	1600	nM	CHEMBL4538975
5.80	IC50	1600	nM	CHEMBL4571967
5.80	IC50	1600	nM	CHEMBL4559227
5.77	IC50	1700	nM	CHEMBL4591202
5.77	IC50	1700	nM	CHEMBL4538870
5.77	IC50	1700	nM	CHEMBL4527785
5.75	IC50	1800	nM	CHEMBL3716578
5.75	IC50	1800	nM	CHEMBL4578339
5.72	IC50	1900	nM	CHEMBL3716731

CTD chemical–gene interactions

24 total (human), top 24 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression, increases methylation	3
FR900359	increases phosphorylation	1
triphenyl phosphate	affects expression	1
2,5,2’,5’-tetrachlorobiphenyl	decreases expression	1
sodium arsenite	affects methylation	1
ICG 001	decreases expression	1
abrine	increases expression	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	decreases expression	1
Resveratrol	decreases expression, affects cotreatment	1
Air Pollutants	increases abundance, increases expression	1
Aspirin	increases expression	1
Diazinon	increases methylation	1
Doxorubicin	increases expression	1
Estradiol	affects cotreatment, increases expression	1
Folic Acid	decreases expression	1
Lead	affects expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Tobacco Smoke Pollution	decreases expression	1
Triclosan	increases expression	1
Aflatoxin B1	increases methylation	1
Okadaic Acid	decreases expression	1
Copper Sulfate	increases expression	1
S-Nitrosoglutathione	decreases expression	1
Particulate Matter	increases abundance, increases expression	1

ChEMBL screening assays

3 unique, capped per target: 3 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4476963	Binding	Inhibition of N-terminal His-tagged and N-terminal alpha-helix lacking Arf6 (14 to 175 residues) (unknown origin) expressed in Escherichia coli using 20 nM Arf6 in presence of ARNO (50 to 255 residues) incubated for 1 hr by fluorometric hig	Arf6 inhibitors and methods of synthesis and use thereof

Clinical trials (associated diseases)

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