FABP5

Summary

FABP5 (fatty acid binding protein 5, HGNC:3560) is a protein-coding gene on chromosome 8q21.13, encoding Fatty acid-binding protein 5 (Q01469). Intracellular carrier for long-chain fatty acids and related active lipids, such as endocannabinoids, that regulate the metabolism and actions of the ligands they bind.

This gene encodes the fatty acid binding protein found in epidermal cells, and was first identified as being upregulated in psoriasis tissue. Fatty acid binding proteins are a family of small, highly conserved, cytoplasmic proteins that bind long-chain fatty acids and other hydrophobic ligands. FABPs may play roles in fatty acid uptake, transport, and metabolism. Polymorphisms in this gene are associated with type 2 diabetes. The human genome contains many pseudogenes similar to this locus.

Source: NCBI Gene 2171 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 25 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001444

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3560
Approved symbol	FABP5
Name	fatty acid binding protein 5
Location	8q21.13
Locus type	gene with protein product
Status	Approved
Aliases	E-FABP, PA-FABP, KFABP
Ensembl gene	ENSG00000164687
Ensembl biotype	protein_coding
OMIM	605168
Entrez	2171

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 6 protein_coding, 2 retained_intron

ENST00000297258, ENST00000396359, ENST00000481695, ENST00000486269, ENST00000917311, ENST00000917312, ENST00000943582, ENST00000943583

RefSeq mRNA: 1 — MANE Select: NM_001444 NM_001444

CCDS: CCDS6228

Canonical transcript exons

ENST00000297258 — 4 exons

Exon	Start	End
ENSE00001086607	81283873	81283974
ENSE00001163337	81280536	81280674
ENSE00003606453	81283366	81283538
ENSE00003851074	81284514	81284775

Expression profiles

Bgee: expression breadth ubiquitous, 141 present calls, max score 99.94.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 87.0237 / max 5695.4528, expressed in 1767 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
89541	84.1181	1757
89540	2.6842	1278
89539	0.2215	89

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
lower esophagus mucosa	UBERON:0035834	99.94	gold quality
esophagus mucosa	UBERON:0002469	99.89	gold quality
ventricular zone	UBERON:0003053	99.84	gold quality
embryo	UBERON:0000922	99.70	gold quality
ganglionic eminence	UBERON:0004023	99.70	gold quality
skin of leg	UBERON:0001511	99.63	gold quality
zone of skin	UBERON:0000014	99.60	gold quality
skin of abdomen	UBERON:0001416	99.56	gold quality
omental fat pad	UBERON:0010414	99.43	gold quality
apex of heart	UBERON:0002098	99.40	gold quality
adipose tissue	UBERON:0001013	99.37	gold quality
subcutaneous adipose tissue	UBERON:0002190	99.32	gold quality
mucosa of transverse colon	UBERON:0004991	99.32	gold quality
placenta	UBERON:0001987	99.20	gold quality
rectum	UBERON:0001052	99.03	gold quality
vagina	UBERON:0000996	99.00	gold quality
esophagus	UBERON:0001043	98.99	gold quality
cortical plate	UBERON:0005343	98.95	gold quality
heart left ventricle	UBERON:0002084	98.94	gold quality
lymph node	UBERON:0000029	98.86	gold quality
hypothalamus	UBERON:0001898	98.80	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	98.73	gold quality
right lung	UBERON:0002167	98.68	gold quality
vermiform appendix	UBERON:0001154	98.65	gold quality
caudate nucleus	UBERON:0001873	98.56	gold quality
colonic epithelium	UBERON:0000397	98.54	gold quality
transverse colon	UBERON:0001157	98.54	gold quality
nucleus accumbens	UBERON:0001882	98.52	gold quality
Ammon’s horn	UBERON:0001954	98.46	gold quality
spleen	UBERON:0002106	98.42	gold quality

Single-cell (SCXA)

Detected in 45 experiment(s), a significant marker in 35.

Experiment	Marker?	Max mean expression
E-MTAB-8142	yes	15347.51
E-HCAD-1	yes	11392.37
E-HCAD-24	yes	4929.06
E-MTAB-9906	yes	4454.52
E-MTAB-10018	yes	4439.74
E-MTAB-8322	yes	3845.58
E-MTAB-8381	yes	1455.49
E-MTAB-6075	yes	1343.37
E-GEOD-81608	yes	875.30
E-GEOD-125970	yes	743.03
E-GEOD-81547	yes	610.11
E-CURD-84	yes	489.92
E-CURD-11	yes	406.44
E-HCAD-4	yes	68.80
E-CURD-122	yes	67.52

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

15 targeting FABP5, 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-6809-3P	99.91	71.45	3814
HSA-MIR-33A-3P	99.70	70.27	3362
HSA-MIR-4729	99.69	72.18	4233
HSA-MIR-603	98.58	68.28	1603
HSA-MIR-1178-3P	98.57	67.09	890
HSA-MIR-216B-3P	98.55	67.19	1223
HSA-MIR-7158-3P	98.46	66.45	728
HSA-MIR-6757-5P	98.08	65.50	724
HSA-MIR-203B-3P	97.82	66.27	979
HSA-MIR-6748-3P	97.20	65.66	836
HSA-MIR-1270	96.94	66.65	931
HSA-MIR-620	96.94	66.79	888
HSA-MIR-4764-3P	96.81	67.94	580
HSA-MIR-6847-3P	96.50	67.30	582
HSA-MIR-549A-5P	96.35	68.08	587

Literature-anchored findings (GeneRIF, showing 40)

• Solution structure and backbone dynamics (PMID:12049637)
• S100A7 expression appears to stabilize epidermal fatty acid binding protein level in keratinocytes (PMID:12839573)
• the overexpression of FABP in cultured senescent dermal microvascular endothelial cells is closely related to skin aging. (PMID:15335354)
• Metastasis of squamous cell carcinoma of the oral tongue is associated with down-regulation of epidermal fatty acid binding protein (E-FABP). (PMID:16759896)
• E-FABP may play a key role in the progress of invasiveness and metastasis in human breast cancer. (PMID:17428383)
• study found levels of nuclear & cytoplasmic C-FABP expression in prostate cancer cells were significantly higher than those in normal & benign prostatic hyperplasia tissues & increased C-FABP was significantly associated with reduced patient survival time (PMID:18360704)
• Results demonstrated the ubiquitous overexpressions of E-FABP and CAPS in EC and the correlations to the clinicopathologic parameters. CAPS might be a potential prognostic factor for survival in patients with endometrial cancer (PMID:18729184)
• epidermal-fatty acid binding protein is upregulated in Human papillomavirus related oral squamous cell carcinoma (PMID:19337991)
• fatty acid-binding protein-5, squamous cell carcinoma antigens 2, alpha-enolase, annexin II, apolipoprotein A-I and albumin were detected at a high level in Atopic dermatitis skin lesions, but scarcely in the normal controls (PMID:19339807)
• FABP5 plays a critical role in lipid metabolism in retinal pigment epithetlial cells; knockdown results in accumulation of cellular triglycerides, decreased cholesterol levels, and reduced secretion of apoB100 protein and lipoproteins (PMID:19434059)
• brain-expressed fatty-acid binding protein (FABP) genes 3, 5 and 7 may have roles in schizophrenia and bipolar disorder (PMID:19554614)
• FABP5 could be a regulated target of Nurr1. (PMID:19861119)
• Overexpression of FABP5 in oral cancer cells increased cell proliferation and invasiveness by increasing expression of MMP-9. (PMID:20040021)
• Fatty acid-binding protein 5 and PPARbeta/delta are critical mediators of epidermal growth factor receptor-induced carcinoma cell growth (PMID:20424164)
• Co-expression of E- and A-FABP is detected in cultured human aortic endothelial cells, which is the critical cellular component in the development of atherosclerosis. (PMID:20452069)
• Studies indicate that three of the ten mammalian FABPs identified to date (FABP3, FABP5, FABP7) are expressed in the brain. (PMID:20563994)
• These results validate the differential expressions of SOD2, S100A8 and FABP5 between mycosis fungoides tissues and normal skins. (PMID:20833513)
• The findings suggest a potential distinct role(s) of SNPs in FABP5 and FABP2 genes in T2DM in different populations. (PMID:21288588)
• The purpose of this study was to investigate the clinicopathological significance of FABP5 in breast cancer and to evaluate FABP5 as a prognostic marker and a possible novel therapeutic target in breast cancer. (PMID:21356353)
• while both serum A-FABP and E-FABP levels are associated with MetS, only A-FABP is significantly associated with increased risk of CAD in Chinese adults (PMID:21492859)
• High FABP5 is associated with pancreatic ductal adenocarcinoma. (PMID:22010213)
• The most significant discovery of the integrated validation is the down-regulation of FABP5 and PDCD4 in KRAS-activated human tumor bronchial epithelial cells. (PMID:22761399)
• FABP5 is significantly overexpressed in intrahepatic cholangiocarcinoma combined lymph node metastasis and is involved in cell proliferation and invasion (PMID:22825302)
• E-FABP levels in skin-strippings, but not in serum, were higher in psoriatic patients than in healthy individuals. E-FABP was abundant in patients not only in lesions but also in uninvolved skin. (PMID:23039948)
• E-FABP showed high exp ression in NSCLC, and the increased E-FABP expression may involved in the occurrence and development of NSCLC (PMID:23327868)
• E-FABP is highly expressed in psoriatic epidermis, and it is mainly localized in stratum spinosum. Psoriatic keratinocytes overexpress E-FABP as compared to the same population in normal epidermis. (PMID:23528210)
• Our findings establish that FABP5 is critical for mammary tumor development (PMID:23722546)
• Both C-FABP and PPARg are suitable as prognostic factors to predict the clinical outcome of prostatic cancer patients. (PMID:24189640)
• peripheral uptake of FA via capillary endothelial FABP4/5 is crucial for systemic metabolism and may establish FABP4/5 as potentially novel targets for the modulation of energy homeostasis. (PMID:24244493)
• Data indicate that fatty acid-binding protein 5 (FABP5) is tuned to selectively stimulate peroxisome proliferation-activated receptor beta/delta transactivation in response to specific fatty acids based on their structural features. (PMID:24692551)
• The frameshift and missense mutations in FABP3, FABP5, and FABP7 genes have been identified in schizophrenia and autism spectrum disorder in humans and in mouse behavioral studies. (PMID:25027319)
• CRABP-II and FABP5 expression patterns are neither related to the tumor grades nor correlated with RA sensitivity. (PMID:25797252)
• FABP5 may contribute to the airway remodeling and inflammation in asthma by fine-tuning the levels of CysLTs, which induce VEGF production. (PMID:26020772)
• Long chain fatty acids suppress the oncogenic properties of FABP5-expressing carcinoma cells in cultured cells. (PMID:26592976)
• silencing of Sp1, c-Myc or FABP5 expression led to a significant decrease in cell proliferation, indicating that up-regulation of FABP5 expression by Sp1 and c-Myc is critical for the proliferation of prostate cancer cells (PMID:26614767)
• the balance between FABP4 and FABP5 in endothelial cells may be important in regulation of angiogenic versus quiescent phenotypes in blood vessels. (PMID:26625874)
• FABP5 promoted VEGF expression and angiogenesis through PPARgamma which was activated by fatty acids transported by FABP5. (PMID:26814431)
• FABP5 is associated with increased subclinical atherosclerosis (PMID:27055964)
• A high expression ratio between FABP5 and CRABPII may be related to CP tumor recurrence and ATRA could be a potential therapeutic agent for CP chemotherapy. (PMID:27418530)
• FABP5 plays an important role in the carcinogenesis and metastasis of cervical cancer, and FABP5 may be a novel predictor for prognostic assessment of cervical cancer patients. (PMID:27644245)

Cross-species orthologs

11 orthologs

Organism	Symbol	Gene ID
danio_rerio	fabp4b	ENSDARG00000002311
danio_rerio	fabp4a	ENSDARG00000017299
danio_rerio	rbp7a	ENSDARG00000091906
danio_rerio	rbp5	ENSDARG00000101481
danio_rerio		ENSDARG00000109259
mus_musculus	Fabp5	ENSMUSG00000027533
rattus_norvegicus	Fabp5	ENSRNOG00000049075
rattus_norvegicus		ENSRNOG00000071720
drosophila_melanogaster	fabp	FBGN0037913
caenorhabditis_elegans		WBGENE00002259
caenorhabditis_elegans		WBGENE00002260

Paralogs (15): RBP2 (ENSG00000114113), RBP1 (ENSG00000114115), FABP3 (ENSG00000121769), RBP5 (ENSG00000139194), CRABP2 (ENSG00000143320), FABP2 (ENSG00000145384), PMP2 (ENSG00000147588), RBP7 (ENSG00000162444), FABP1 (ENSG00000163586), FABP7 (ENSG00000164434), CRABP1 (ENSG00000166426), FABP6 (ENSG00000170231), FABP4 (ENSG00000170323), FABP12 (ENSG00000197416), FABP9 (ENSG00000205186)

Protein

Protein identifiers

Fatty acid-binding protein 5 — Q01469 (reviewed: Q01469)

Alternative names: Epidermal-type fatty acid-binding protein, Fatty acid-binding protein, epidermal, Psoriasis-associated fatty acid-binding protein homolog

All UniProt accessions (3): Q01469, E7DVW5, I6L8B7

UniProt curated annotations — full annotation on UniProt →

Function. Intracellular carrier for long-chain fatty acids and related active lipids, such as endocannabinoids, that regulate the metabolism and actions of the ligands they bind. In addition to the cytosolic transport, selectively delivers specific fatty acids from the cytosol to the nucleus, wherein they activate nuclear receptors. Delivers retinoic acid to the nuclear receptor peroxisome proliferator-activated receptor delta; which promotes proliferation and survival. May also serve as a synaptic carrier of endocannabinoid at central synapses and thus controls retrograde endocannabinoid signaling. Modulates inflammation by regulating PTGES induction via NF-kappa-B activation, and prostaglandin E2 (PGE2) biosynthesis during inflammation. May be involved in keratinocyte differentiation.

Subunit / interactions. Monomer. Homodimer.

Subcellular location. Cytoplasm. Nucleus. Synapse. Postsynaptic density. Secreted.

Tissue specificity. Keratinocytes; highly expressed in psoriatic skin. Expressed in brain gray matter.

Domain organisation. Forms a beta-barrel structure that accommodates the hydrophobic ligand in its interior.

Similarity. Belongs to the calycin superfamily. Fatty-acid binding protein (FABP) family.

RefSeq proteins (1): NP_001435* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000463	Fatty_acid-bd	Domain
IPR000566	Lipocln_cytosolic_FA-bd_dom	Domain
IPR012674	Calycin	Homologous_superfamily
IPR031259	ILBP	Family

Pfam: PF00061

Catalyzed reactions (Rhea), 3 shown:

• (9Z)-octadecenoate(out) = (9Z)-octadecenoate(in) (RHEA:33655)
• hexadecanoate(out) = hexadecanoate(in) (RHEA:45256)
• (9Z,12Z)-octadecadienoate(out) = (9Z,12Z)-octadecadienoate(in) (RHEA:45264)

UniProt features (29 total): strand 11, binding site 5, modified residue 3, mutagenesis site 3, helix 3, initiator methionine 1, chain 1, disulfide bond 1, short sequence motif 1

Structure

Experimental structures (PDB)

17 structures.

PDB	Method	Resolution (Å)
7G0E	X-RAY DIFFRACTION	1.11
7G01	X-RAY DIFFRACTION	1.17
7G1Q	X-RAY DIFFRACTION	1.24
7FY0	X-RAY DIFFRACTION	1.34
5HZ5	X-RAY DIFFRACTION	1.4
7G04	X-RAY DIFFRACTION	1.4
7FYD	X-RAY DIFFRACTION	1.45
7G0B	X-RAY DIFFRACTION	1.47
4LKP	X-RAY DIFFRACTION	1.67
7FWI	X-RAY DIFFRACTION	2
1B56	X-RAY DIFFRACTION	2.05
5UR9	X-RAY DIFFRACTION	2.2
7FXD	X-RAY DIFFRACTION	2.44
4LKT	X-RAY DIFFRACTION	2.57
4AZM	X-RAY DIFFRACTION	2.75
4AZR	X-RAY DIFFRACTION	2.95
1JJJ	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q01469-F1	96.46	0.96

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 (5): 43; 109; 129–131; 131; 131

Post-translational modifications (3): 131, 2, 17

Disulfide bonds (1): 120–127

Mutagenesis-validated functional residues (3):

Position	Phenotype
24	loss of ligand-induced nuclear import; when associated with a-33 and a-34.
33	loss of ligand-induced nuclear import; when associated with a-24 and a-34.
34	loss of ligand-induced nuclear import; when associated with a-24 and a-33.

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-163560	Triglyceride catabolism
R-HSA-5362517	Signaling by Retinoic Acid
R-HSA-6798695	Neutrophil degranulation
R-HSA-9725554	Differentiation of Keratinocytes in Interfollicular Epidermis in Mammalian Skin

MSigDB gene sets: 509 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_DN, GSE18804_SPLEEN_MACROPHAGE_VS_BRAIN_TUMORAL_MACROPHAGE_DN, GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_DN, GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_DN, REACTOME_TRIGLYCERIDE_CATABOLISM, GOBP_NEGATIVE_REGULATION_OF_TRANSMEMBRANE_TRANSPORT, GOBP_CARBOHYDRATE_TRANSPORT, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, REACTOME_INNATE_IMMUNE_SYSTEM, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_BIOSYNTHETIC_PROCESS, GOCC_SECRETORY_GRANULE, MODULE_151

GO Biological Process (16): glucose metabolic process (GO:0006006), lipid metabolic process (GO:0006629), phosphatidylcholine biosynthetic process (GO:0006656), epidermis development (GO:0008544), negative regulation of D-glucose transmembrane transport (GO:0010829), fatty acid transport (GO:0015908), long-chain fatty acid transport (GO:0015909), regulation of prostaglandin biosynthetic process (GO:0031392), positive regulation of peroxisome proliferator activated receptor signaling pathway (GO:0035360), glucose homeostasis (GO:0042593), regulation of sensory perception of pain (GO:0051930), retrograde trans-synaptic signaling by endocannabinoid (GO:0098921), regulation of retrograde trans-synaptic signaling by endocanabinoid (GO:0099178), positive regulation of cold-induced thermogenesis (GO:0120162), lipid transport across blood-brain barrier (GO:1990379), lipid transport (GO:0006869)

GO Molecular Function (6): retinoic acid binding (GO:0001972), long-chain fatty acid transmembrane transporter activity (GO:0005324), fatty acid binding (GO:0005504), lipid binding (GO:0008289), identical protein binding (GO:0042802), protein binding (GO:0005515)

GO Cellular Component (15): extracellular region (GO:0005576), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), postsynaptic density (GO:0014069), secretory granule membrane (GO:0030667), azurophil granule lumen (GO:0035578), synapse (GO:0045202), extracellular exosome (GO:0070062), glutamatergic synapse (GO:0098978), postsynaptic density, intracellular component (GO:0099092), postsynaptic cytosol (GO:0099524), obsolete extracellular space (GO:0005615)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
Triglyceride metabolism	1
Signaling by Nuclear Receptors	1
Innate Immune System	1
Developmental Cell Lineages of the Integumentary System	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
lipid transport	2
monocarboxylic acid binding	2
binding	2
hexose metabolic process	1
primary metabolic process	1
phosphatidylcholine metabolic process	1
glycerophospholipid biosynthetic process	1
tissue development	1
regulation of D-glucose transmembrane transport	1
negative regulation of transmembrane transport	1
D-glucose transmembrane transport	1
monocarboxylic acid transport	1
fatty acid transport	1
prostaglandin biosynthetic process	1
regulation of unsaturated fatty acid biosynthetic process	1
peroxisome proliferator activated receptor signaling pathway	1
regulation of peroxisome proliferator activated receptor signaling pathway	1
positive regulation of intracellular signal transduction	1
carbohydrate homeostasis	1
sensory perception of pain	1
regulation of sensory perception	1
retrograde trans-synaptic signaling by lipid	1
trans-synaptic signaling by endocannabinoid	1
retrograde trans-synaptic signaling by endocannabinoid	1
regulation of trans-synaptic signaling	1
positive regulation of multicellular organismal process	1
cold-induced thermogenesis	1
regulation of cold-induced thermogenesis	1
transport across blood-brain barrier	1
transport	1
lipid localization	1
retinoid binding	1
fatty acid transmembrane transporter activity	1
long-chain fatty acid transport	1
lipid binding	1
protein binding	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
intracellular anatomical structure	1

Protein interactions and networks

STRING

2004 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FABP5	PPARD	Q03181	978
FABP5	FAAH	O00519	891
FABP5	GOT2	P00505	888
FABP5	S100A7	P31151	770
FABP5	CD36	P16671	744
FABP5	PPARG	P37231	740
FABP5	SCARB1	Q8WTV0	737
FABP5	SCARB2	Q14108	737
FABP5	NOTCH3	Q9UM47	702
FABP5	PPARA	Q07869	700
FABP5	FABP6	P51161	596
FABP5	RARA	P10276	572
FABP5	ESRRA	P11474	571
FABP5	FASN	P49327	571
FABP5	FN1	P02751	532

IntAct

69 interactions, top by confidence:

A	B	Type	Score
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
ASF1A	HAT1	psi-mi:“MI:0914”(association)	0.640
ASF1B	HAT1	psi-mi:“MI:0914”(association)	0.640
NASP	HAT1	psi-mi:“MI:0914”(association)	0.530
	CD5L	psi-mi:“MI:0915”(physical association)	0.400
KSR1	FBLL1	psi-mi:“MI:0914”(association)	0.350
LRRK2		psi-mi:“MI:0914”(association)	0.350
SLX4	MYO1C	psi-mi:“MI:0914”(association)	0.350
BAZ2A	CSTA	psi-mi:“MI:0914”(association)	0.350
KDM3B	CPNE3	psi-mi:“MI:0914”(association)	0.350
KRR1	LGALS7	psi-mi:“MI:0914”(association)	0.350
NEDD4	HMGB1P1	psi-mi:“MI:0914”(association)	0.350
NELFB	PRSS3	psi-mi:“MI:0914”(association)	0.350
NELFCD	H1-2	psi-mi:“MI:0914”(association)	0.350
NELFE	H1-2	psi-mi:“MI:0914”(association)	0.350
PIWIL4	CSTA	psi-mi:“MI:0914”(association)	0.350
RAD51	CSTA	psi-mi:“MI:0914”(association)	0.350
TDRD5	UBB	psi-mi:“MI:0914”(association)	0.350
TRIM24	DDTL	psi-mi:“MI:0914”(association)	0.350
P		psi-mi:“MI:0914”(association)	0.350
TIFAB	DDX3X	psi-mi:“MI:0914”(association)	0.350
pipB2	PSMD12	psi-mi:“MI:0914”(association)	0.350
MSH2	GGCT	psi-mi:“MI:0914”(association)	0.350
MAPT	SHTN1	psi-mi:“MI:0914”(association)	0.350

BioGRID (173): FABP5 (Affinity Capture-MS), FABP5 (Affinity Capture-MS), AKR1B1 (Co-fractionation), ECI1 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation), FABP5 (Co-fractionation)

ESM2 similar proteins: A0A0K0MJ13, A0A0K0MJN3, A6YLM6, C4N147, O01812, O01814, O02772, O08716, O13008, O15540, O45035, O97788, P02689, P02690, P02691, P04117, P05413, P06768, P07483, P0C6G6, P10790, P11404, P15090, P24526, P29498, P41496, P41509, P48035, P50120, P50121, P51880, P55051, P55052, P55053, P70623, P80049, P86412, Q01469, Q02970, Q05423

Diamond homologs: A0A0K0MJ13, A0A0K0MJN3, A6NFH5, A6YLM6, A8MUU1, B7SUM8, C4N147, O01812, O01814, O02323, O02324, O02772, O08716, O13008, O15540, O42386, O45035, O76821, O97788, P02689, P02690, P02691, P02694, P02696, P04117, P05413, P06768, P07148, P07483, P09455, P0C6G6, P10790, P11404, P12710, P15090, P22935, P24526, P29373, P29498, P29762

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
FABP5	“up-regulates quantity”	“Fatty acid”	relocalization

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 82 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.

GO biological processes:

GO term	Partners	Fold	FDR
negative regulation of transcription elongation by RNA polymerase II	5	52.5×	3e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	17
Likely benign	0
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

0 predictions. Top by Δscore:

AlphaMissense

890 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
8:81280650:T:C	F19L	0.998
8:81280652:T:A	F19L	0.998
8:81280652:T:G	F19L	0.998
8:81283529:A:C	R81S	0.998
8:81283529:A:T	R81S	0.998
8:81283947:A:C	R109S	0.997
8:81283947:A:T	R109S	0.997
8:81280626:T:A	W11R	0.996
8:81280626:T:C	W11R	0.996
8:81283521:G:C	D79H	0.996
8:81283528:G:C	R81T	0.996
8:81284540:T:G	C127W	0.996
8:81283946:G:C	R109T	0.995
8:81284545:G:C	R129P	0.995
8:81280628:G:C	W11C	0.994
8:81280628:G:T	W11C	0.994
8:81283458:A:C	S58R	0.994
8:81283460:C:A	S58R	0.994
8:81283460:C:G	S58R	0.994
8:81283522:A:T	D79V	0.994
8:81283933:A:C	S105R	0.994
8:81283935:C:A	S105R	0.994
8:81283935:C:G	S105R	0.994
8:81284538:T:C	C127R	0.994
8:81280664:G:A	M23I	0.993
8:81280664:G:C	M23I	0.993
8:81280664:G:T	M23I	0.993
8:81283523:T:A	D79E	0.993
8:81283523:T:G	D79E	0.993
8:81283901:T:C	L94S	0.993

dbSNP variants (sampled 300 via entrez): RS1000184253 (8:81281642 G>C), RS1000320624 (8:81280437 G>A,T), RS1001338971 (8:81284894 A>G), RS1001614661 (8:81281089 C>A), RS1001918089 (8:81280906 A>G,T), RS1003061798 (8:81283293 G>A,T), RS1003184640 (8:81282167 A>T), RS1003361203 (8:81282130 G>A,T), RS1003438724 (8:81283709 C>G), RS1003689084 (8:81282625 T>A), RS1003798540 (8:81281682 A>G), RS1004928546 (8:81283825 C>G,T), RS1005188612 (8:81279717 T>A), RS1005401500 (8:81282585 A>G), RS1006131560 (8:81284961 G>C)

Disease associations

OMIM: gene MIM:605168 | 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): CHEMBL3674 (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: 713,838 (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
CHEMBL8659	OLEIC ACID	2	713,838

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — Fatty acid-binding proteins

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
compound 13 [PMID: 17502136]	Inhibition	8.7	pKi

Binding affinities (BindingDB)

314 measured of 369 human assays (369 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	10 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	10 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-4,4-dimethyl-6,7-dihydro-5H-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	10 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[6-ethyl-3-(4-methyl-1,3-thiazol-2-yl)-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	10 nM	US-9604977: Bicyclic thiophenylamide compounds
US20250325529, ID PD154	KD	11 nM	US-20250325529: INHIBITORS OF FATTY ACID BINDING PROTEINS (FABPs), METHODS OF USE AND METHODS OF MAKING
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6-ethyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	13 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[(6S)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6-ethyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	13 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[5-cyclopropyl-3-(3-cyclopropyl-1,2,4-thiadiazol-5-yl)-4-methylthiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	16 nM	US-9353102: Non-annulated thiophenylamides
US20250325529, ID PD151	KD	16 nM	US-20250325529: INHIBITORS OF FATTY ACID BINDING PROTEINS (FABPs), METHODS OF USE AND METHODS OF MAKING
2-[[(6R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6-ethyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	18 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]-4,4-dimethylcyclopentene-1-carboxylic acid	IC50	19 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-[3-(trifluoromethyl)-1,2,4-oxadiazol-5-yl]-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	20 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[4,4-dimethyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)-5,6-dihydrocyclopenta[b]thiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	20 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-[4-(trifluoromethyl)-1,3-thiazol-2-yl]-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	20 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-[4-(trifluoromethyl)-1,3-thiazol-2-yl]-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	20 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	20 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[(6S)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	20 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[6,6-difluoro-3-[3-(trifluoromethyl)-1,2,4-oxadiazol-5-yl]-5,7-dihydro-4H-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	20 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[6,6-difluoro-3-(4-methyl-1,3-thiazol-2-yl)-5,7-dihydro-4H-1-benzothiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	20 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[3-(3-cyclopropyl-1,2,4-thiadiazol-5-yl)-4,5-dimethylthiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	22 nM	US-9353102: Non-annulated thiophenylamides
2-[[5-cyclopropyl-3-(3-cyclopropyl-1,2,4-thiadiazol-5-yl)-4-methylthiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	22 nM	US-9353102: Non-annulated thiophenylamides
2-[[3-(4-methyl-1,3-thiazol-2-yl)-6-(trifluoromethyl)-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	22 nM	US-9604977: Bicyclic thiophenylamide compounds
US20250325529, ID PD152	KD	28 nM	US-20250325529: INHIBITORS OF FATTY ACID BINDING PROTEINS (FABPs), METHODS OF USE AND METHODS OF MAKING
2-[[5-cyclopropyl-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-4-methylthiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9353102: Non-annulated thiophenylamides
2-[[4-cyclopropyl-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-5-methylthiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9353102: Non-annulated thiophenylamides
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-4,5-dimethylthiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9353102: Non-annulated thiophenylamides
2-[[4-cyclopropyl-5-methyl-3-[3-(trifluoromethyl)-1,2,4-oxadiazol-5-yl]thiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9353102: Non-annulated thiophenylamides
2-[[5-cyclopropyl-4-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)thiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9353102: Non-annulated thiophenylamides
3-[[3-[3-(trifluoromethyl)-1,2,4-oxadiazol-5-yl]-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-1-benzothiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[3-[4-(trifluoromethyl)-1,3-thiazol-2-yl]-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-4,4-dimethyl-6,7-dihydro-5H-1-benzothiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[5-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3-thiatricyclo[5.2.1.02,6]deca-2(6),4-dien-4-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-[3-(trifluoromethyl)-1,2,4-oxadiazol-5-yl]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[3-[3-(trifluoromethyl)-1,2,4-oxadiazol-5-yl]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-5,6-dihydro-4H-cyclopenta[b]thiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6,6-difluoro-5,7-dihydro-4H-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[6,6-difluoro-3-(4-methyl-1,3-thiazol-2-yl)-5,7-dihydro-4H-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-thiadiazol-5-yl)-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[6,6-difluoro-3-(4-propan-2-yl-1,3-thiazol-2-yl)-5,7-dihydro-4H-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	30 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[5-cyclopropyl-4-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)thiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	31 nM	US-9353102: Non-annulated thiophenylamides
2-[[4,5-dimethyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)thiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	31 nM	US-9353102: Non-annulated thiophenylamides
3-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-6-ethyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	32 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[(6S)-6-ethyl-3-(4-methyl-1,3-thiazol-2-yl)-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	32 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-thiadiazol-5-yl)-6,6-difluoro-5,7-dihydro-4H-1-benzothiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	33 nM	US-9604977: Bicyclic thiophenylamide compounds
3-[[3-(3-cyclopropyl-1,2,4-thiadiazol-5-yl)-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]carbamoyl]bicyclo[2.2.2]oct-2-ene-2-carboxylic acid	IC50	34 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[5-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3,4-dihydro-2H-thieno[2,3-b]pyran-6-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	34 nM	US-9604977: Bicyclic thiophenylamide compounds
2-[[3-(3-cyclopropyl-1,2,4-thiadiazol-5-yl)-4,5-dimethylthiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	38 nM	US-9353102: Non-annulated thiophenylamides
2-[[3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-5,5-dimethyl-6,7-dihydro-4H-1-benzothiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	38 nM	US-9604977: Bicyclic thiophenylamide compounds

ChEMBL bioactivities

422 potent at pChembl≥5 of 488 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.70	Ki	2	nM	CHEMBL247298
8.52	Ki	3	nM	CHEMBL212860
8.05	Ki	9	nM	CHEMBL437489
8.00	IC50	10	nM	CHEMBL5820726
8.00	IC50	10	nM	CHEMBL5818769
8.00	IC50	10	nM	CHEMBL6036857
8.00	IC50	10	nM	CHEMBL5887095
7.89	IC50	13	nM	CHEMBL5827983
7.89	IC50	13	nM	CHEMBL5759517
7.80	IC50	16	nM	CHEMBL3923099
7.75	IC50	18	nM	CHEMBL5769424
7.72	IC50	19	nM	CHEMBL5922908
7.70	IC50	20	nM	CHEMBL5278217
7.70	IC50	20	nM	CHEMBL6040071
7.70	IC50	20	nM	CHEMBL5872622
7.70	IC50	20	nM	CHEMBL5848566
7.70	IC50	20	nM	CHEMBL5745897
7.70	IC50	20	nM	CHEMBL5987784
7.70	IC50	20	nM	CHEMBL5821426
7.70	IC50	20	nM	CHEMBL5872270
7.70	IC50	20	nM	CHEMBL5957565
7.66	IC50	22	nM	CHEMBL3920801
7.66	IC50	22	nM	CHEMBL3914116
7.66	IC50	22	nM	CHEMBL5813196
7.52	IC50	30	nM	CHEMBL3918729
7.52	IC50	30	nM	CHEMBL3896498
7.52	IC50	30	nM	CHEMBL3919426
7.52	IC50	30	nM	CHEMBL3957282
7.52	IC50	30	nM	CHEMBL3896829
7.52	IC50	30	nM	CHEMBL5287082
7.52	IC50	30	nM	CHEMBL5912944
7.52	IC50	30	nM	CHEMBL5787607
7.52	IC50	30	nM	CHEMBL5781926
7.52	IC50	30	nM	CHEMBL5805611
7.52	IC50	30	nM	CHEMBL6064445
7.52	IC50	30	nM	CHEMBL5820174
7.52	IC50	30	nM	CHEMBL5929433
7.52	IC50	30	nM	CHEMBL5992918
7.52	IC50	30	nM	CHEMBL5836763
7.52	IC50	30	nM	CHEMBL5932782
7.52	IC50	30	nM	CHEMBL5771767
7.52	IC50	30	nM	CHEMBL5760016
7.52	IC50	30	nM	CHEMBL6009768
7.51	IC50	31	nM	CHEMBL3938613
7.51	IC50	31	nM	CHEMBL3986878
7.50	IC50	32	nM	CHEMBL5808252
7.50	IC50	32	nM	CHEMBL5770936
7.48	Ki	33	nM	CHEMBL378857
7.48	IC50	33	nM	CHEMBL5957946
7.47	IC50	34	nM	CHEMBL6052767

PubChem BioAssay actives

159 with measured affinity, of 346 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
2-[2,3-bis[(2-chlorophenyl)methoxy]phenyl]-2-oxoacetic acid	268957: Binding affinity to human kFABP	ki	0.0020	uM
2,3-bis[(2,4-dichloro-3-tritiophenyl)methoxy]benzoic acid	307909: Displacement of 1,8-ANS from eFABP by fluorescence based-assay	ki	0.0020	uM
2-[2,3-bis[(2-chlorophenyl)methoxy]phenyl]acetic acid	268957: Binding affinity to human kFABP	ki	0.0030	uM
2-[2,3-bis[(2-chlorophenyl)methoxy]phenyl]-2-methoxyacetic acid	268957: Binding affinity to human kFABP	ki	0.0090	uM
2-[1-(methoxymethyl)cyclopentyl]-6-pentyl-4-phenyl-3-(2H-tetrazol-5-yl)-5,6,7,8-tetrahydroquinoline	1958767: Inhibition of human FABP5	ic50	0.0200	uM
[1-[4-(2-methyl-4-pyridinyl)-3-(2H-tetrazol-5-yl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-2-yl]cyclopentyl]methanol	1958767: Inhibition of human FABP5	ic50	0.0300	uM
(2S)-2-[2,3-bis[(2-chlorophenyl)methoxy]phenyl]-2-hydroxyacetic acid	268957: Binding affinity to human kFABP	ki	0.0330	uM
2-(1-methylcyclopentyl)-4-(2-methyl-4-pyridinyl)-3-(2H-tetrazol-5-yl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine	1958767: Inhibition of human FABP5	ic50	0.0400	uM
6-chloro-N,N-diethyl-7-fluoro-4-phenyl-3-(2H-tetrazol-5-yl)quinolin-2-amine	1958768: Inhibition of FABP5 (unknown origin)	ic50	0.0510	uM
6-chloro-7-fluoro-4-phenyl-2-piperidin-1-yl-3-(2H-tetrazol-5-yl)quinoline	1958768: Inhibition of FABP5 (unknown origin)	ic50	0.0620	uM
N,N-diethyl-4-phenyl-3-(2H-tetrazol-5-yl)-6-(trifluoromethyl)quinolin-2-amine	1958768: Inhibition of FABP5 (unknown origin)	ic50	0.0640	uM
2-cyclopentyl-6-methyl-4-(2-methyl-4-pyridinyl)-3-(2H-tetrazol-5-yl)-5,6,7,8-tetrahydroquinoline	1958767: Inhibition of human FABP5	ic50	0.0700	uM
6-chloro-7-fluoro-2-pentan-3-yl-4-phenyl-3-(2H-tetrazol-5-yl)quinoline	1958768: Inhibition of FABP5 (unknown origin)	ic50	0.0800	uM
6-chloro-4-phenyl-2-piperidin-1-yl-3-(2H-tetrazol-5-yl)quinoline	1322080: Displacement of Bodipy-labeled fatty acid from human N-terminal His6-tagged FABP5 (127 to 132 residues) expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.0860	uM
2-cyclohexyl-4-(2-methyl-4-pyridinyl)-3-(2H-tetrazol-5-yl)-6-(trifluoromethyl)-5,6,7,8-tetrahydroquinoline	1958767: Inhibition of human FABP5	ic50	0.0900	uM
4-phenyl-2-piperidin-1-yl-3-(2H-tetrazol-5-yl)-6-(trifluoromethyl)quinoline	1958768: Inhibition of FABP5 (unknown origin)	ic50	0.0960	uM
6-chloro-8-methyl-4-phenyl-2-piperidin-1-ylquinoline-3-carboxylic acid	1322080: Displacement of Bodipy-labeled fatty acid from human N-terminal His6-tagged FABP5 (127 to 132 residues) expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.1000	uM
trans-(2S,4S)-3-[3-(2-oxo-1,3-dihydroindol-6-yl)phenoxy]carbonyl-2,4-diphenylcyclobutane-1-carboxylic acid	2014898: Displacement of fluorescent probe DAUDA from FABP5 (unknown origin) assessed as inhibition constant by fluorescence based microplate reader analysis	ki	0.1200	uM
6,8-dichloro-4-phenyl-2-piperidin-1-ylquinoline-3-carboxylic acid	1322080: Displacement of Bodipy-labeled fatty acid from human N-terminal His6-tagged FABP5 (127 to 132 residues) expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.1200	uM
5-(6-chloro-4-phenyl-2-piperidin-1-ylquinolin-3-yl)-3H-1,3,4-oxadiazole-2-thione	1322080: Displacement of Bodipy-labeled fatty acid from human N-terminal His6-tagged FABP5 (127 to 132 residues) expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.1330	uM
5-(6-chloro-4-phenyl-2-piperidin-1-ylquinolin-3-yl)-3H-1,3,4-oxadiazol-2-one	1322080: Displacement of Bodipy-labeled fatty acid from human N-terminal His6-tagged FABP5 (127 to 132 residues) expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.1670	uM
trans-(2S,4S)-2,4-diphenyl-3-[(1R,2S)-2-phenylcyclohexyl]oxycarbonylcyclobutane-1-carboxylic acid	1404706: Displacement of DAUDA from recombinant human N-terminal His-tagged FABP5 expressed in Escherichia coli BL21(DE3) after 20 mins by fluorescence assay	ki	0.1800	uM
6-chloro-N-ethyl-N-methyl-4-phenyl-3-(2H-tetrazol-5-yl)quinolin-2-amine	1958768: Inhibition of FABP5 (unknown origin)	ic50	0.1820	uM
6,8-dichloro-2-[ethyl(methyl)amino]-4-phenylquinoline-3-carboxylic acid	1958768: Inhibition of FABP5 (unknown origin)	ic50	0.1830	uM
trans-(2S,4S)-2,4-diphenyl-3-[(1S,2R)-2-phenylcyclohexyl]oxycarbonylcyclobutane-1-carboxylic acid	1404706: Displacement of DAUDA from recombinant human N-terminal His-tagged FABP5 expressed in Escherichia coli BL21(DE3) after 20 mins by fluorescence assay	ki	0.2000	uM
3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]benzoic acid	307909: Displacement of 1,8-ANS from eFABP by fluorescence based-assay	ki	0.2400	uM
(Z)-octadec-9-enoic acid	307909: Displacement of 1,8-ANS from eFABP by fluorescence based-assay	ki	0.2480	uM
2-[3-[2-(3-ethyl-4,5-diphenylfuran-2-yl)phenyl]phenoxy]acetic acid	307909: Displacement of 1,8-ANS from eFABP by fluorescence based-assay	ki	0.2900	uM
trans-(2S,4S)-3-(2-cyano-5-phenylphenoxy)carbonyl-2,4-diphenylcyclobutane-1-carboxylic acid	2014898: Displacement of fluorescent probe DAUDA from FABP5 (unknown origin) assessed as inhibition constant by fluorescence based microplate reader analysis	ki	0.3200	uM
trans-(2S,4S)-3-(2-cyano-5-phenylphenoxy)carbonyl-2,4-bis(2-methoxyphenyl)cyclobutane-1-carboxylic acid	2014898: Displacement of fluorescent probe DAUDA from FABP5 (unknown origin) assessed as inhibition constant by fluorescence based microplate reader analysis	ki	0.3300	uM
2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetic acid	307909: Displacement of 1,8-ANS from eFABP by fluorescence based-assay	ki	0.3500	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148356: Binding affinity to human FABP5 incubated for 45 mins by Kinobead based pull down assay	kd	0.3590	uM
trans-(2S,4S)-3-[3-(1,3-benzodioxol-5-yl)phenoxy]carbonyl-2,4-diphenylcyclobutane-1-carboxylic acid	2014898: Displacement of fluorescent probe DAUDA from FABP5 (unknown origin) assessed as inhibition constant by fluorescence based microplate reader analysis	ki	0.3600	uM
4-[4-fluoro-2-[1-phenyl-5-[2-(trifluoromethyl)phenyl]pyrazol-3-yl]phenoxy]butanoic acid	2082681: Binding affinity FABP5 (unknown origin) assessed as inhibition constant	ki	0.4100	uM
2-[2-(1-benzofuran-5-yl)-3-chloroanilino]benzoic acid	1648409: Displacement of 1,8-ANS from recombinant human 6His-tagged FABP5 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay	ki	0.4300	uM
2-[3-chloro-2-(1H-indazol-5-yl)anilino]benzoic acid	1648409: Displacement of 1,8-ANS from recombinant human 6His-tagged FABP5 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay	ki	0.4900	uM
6-chloro-4-phenyl-2-piperidin-1-ylquinoline-3-carboxylic acid	1949364: Inhibition of FABP5 (unknown origin) assessed as inhibition constant	ki	0.4900	uM
trans-(2R,4R)-3-[(2-cyano-5-phenylphenyl)carbamoyl]-2,4-diphenylcyclobutane-1-carboxylic acid	2014898: Displacement of fluorescent probe DAUDA from FABP5 (unknown origin) assessed as inhibition constant by fluorescence based microplate reader analysis	ki	0.5000	uM
trans-(2S,4S)-2,4-bis(2-methoxyphenyl)-3-naphthalen-1-yloxycarbonylcyclobutane-1-carboxylic acid	1404706: Displacement of DAUDA from recombinant human N-terminal His-tagged FABP5 expressed in Escherichia coli BL21(DE3) after 20 mins by fluorescence assay	ki	0.5500	uM
2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenyl]-2-hydroxyacetic acid	307909: Displacement of 1,8-ANS from eFABP by fluorescence based-assay	ki	0.5500	uM
4-carbazol-9-ylbutanoic acid	2082676: Inhibition of FABP5 (unknown origin)	ic50	0.5700	uM
2-(3-chloro-2-naphthalen-2-ylanilino)benzoic acid	1648409: Displacement of 1,8-ANS from recombinant human 6His-tagged FABP5 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay	ki	0.6000	uM
2-[2-(2,1,3-benzoxadiazol-5-yl)-3-chloroanilino]benzoic acid	1648409: Displacement of 1,8-ANS from recombinant human 6His-tagged FABP5 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay	ki	0.6000	uM
Palmitic Acid	1802832: Ligand Binding Assay from Article 10.1074/jbc.M113.514646: “Structural basis for ligand regulation of the fatty acid-binding protein 5, peroxisome proliferator-activated receptor ß/d (FABP5-PPARß/d) signaling pathway.”	ki	0.6700	uM
trans-(2S,4S)-2,4-bis(2-methoxyphenyl)-3-[(1R,2S)-2-phenylcyclohexyl]oxycarbonylcyclobutane-1-carboxylic acid	1404706: Displacement of DAUDA from recombinant human N-terminal His-tagged FABP5 expressed in Escherichia coli BL21(DE3) after 20 mins by fluorescence assay	ki	0.6800	uM
(1S,2S,3R,6S)-4-(hydroxymethyl)-6-(octylamino)cyclohex-4-ene-1,2,3-triol	1802832: Ligand Binding Assay from Article 10.1074/jbc.M113.514646: “Structural basis for ligand regulation of the fatty acid-binding protein 5, peroxisome proliferator-activated receptor ß/d (FABP5-PPARß/d) signaling pathway.”	ki	0.7000	uM
trans-(2R,4R)-3-naphthalen-1-yloxycarbonyl-2,4-diphenylcyclobutane-1-carboxylic acid	1404706: Displacement of DAUDA from recombinant human N-terminal His-tagged FABP5 expressed in Escherichia coli BL21(DE3) after 20 mins by fluorescence assay	ki	0.7100	uM
trans-(2S,4S)-3-[3-(1,3-benzodioxol-5-yl)phenoxy]carbonyl-2,4-bis(2-methoxyphenyl)cyclobutane-1-carboxylic acid	2014898: Displacement of fluorescent probe DAUDA from FABP5 (unknown origin) assessed as inhibition constant by fluorescence based microplate reader analysis	ki	0.7200	uM
trans-(2R,4R)-3-[[3-(1,3-benzodioxol-5-yl)phenyl]carbamoyl]-2,4-diphenylcyclobutane-1-carboxylic acid	2014898: Displacement of fluorescent probe DAUDA from FABP5 (unknown origin) assessed as inhibition constant by fluorescence based microplate reader analysis	ki	0.7600	uM
trans-(2S,4S)-2,4-diphenyl-3-(2-phenylphenoxy)carbonylcyclobutane-1-carboxylic acid	1404706: Displacement of DAUDA from recombinant human N-terminal His-tagged FABP5 expressed in Escherichia coli BL21(DE3) after 20 mins by fluorescence assay	ki	0.7700	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases expression, decreases methylation, affects cotreatment	8
sodium arsenite	affects expression, decreases expression, increases expression	5
bisphenol A	affects expression, decreases expression, decreases methylation	3
trichostatin A	affects cotreatment, increases expression	3
Cadmium	decreases reaction, increases abundance, increases palmitoylation, increases expression, decreases expression	3
Cadmium Chloride	decreases reaction, increases abundance, increases palmitoylation, decreases expression, increases expression	3
sodium arsenate	decreases expression, increases abundance	2
nickel sulfate	increases expression, decreases expression	2
chloropicrin	increases expression	2
bisphenol S	affects cotreatment, increases methylation, increases expression	2
Benzo(a)pyrene	decreases methylation, increases methylation, decreases expression	2
Dexamethasone	increases expression, affects cotreatment	2
Lead	affects binding, affects expression	2
Tobacco Smoke Pollution	affects expression, increases expression	2
Tretinoin	increases expression, decreases expression	2
GSK-J4	decreases expression	1
4-oxoretinoic acid	decreases expression	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	increases expression	1
pyrogallol 1,3-dimethyl ether	decreases expression, affects cotreatment, affects localization	1
2-methyl-4-isothiazolin-3-one	increases expression	1
terbufos	increases methylation	1
arsenite	affects binding, increases reaction	1
mono-(2-ethylhexyl)phthalate	increases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
cobaltous chloride	decreases expression	1
butyraldehyde	increases expression	1
2-bromopalmitate	increases abundance, increases palmitoylation, decreases reaction	1
perfluorooctanoic acid	decreases expression	1
zinc chromate	decreases expression, increases abundance	1

ChEMBL screening assays

39 unique, capped per target: 39 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1102420	Binding	Displacement of radiolabeled 1-anilinonaphthalene 8-sulfonic acid from EFABP expressed in Escherichia coli BL21 (DE3) by fluorescence spectrophotometry	Identification and characterization of a small molecule inhibitor of Fatty Acid binding proteins. — J Med Chem

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1RS	Abcam HeLa FABP5 KO	Cancer cell line	Female
CVCL_E0YJ	Ubigene MDA-MB-231 FABP5 KO	Cancer cell line	Female

Clinical trials (associated diseases)

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