FABP4

Summary

FABP4 (fatty acid binding protein 4, HGNC:3559) is a protein-coding gene on chromosome 8q21.13, encoding Fatty acid-binding protein, adipocyte (P15090). Lipid transport protein in adipocytes.

FABP4 encodes the fatty acid binding protein found in adipocytes. Fatty acid binding proteins are a family of small, highly conserved, cytoplasmic proteins that bind long-chain fatty acids and other hydrophobic ligands. It is thought that FABPs roles include fatty acid uptake, transport, and metabolism.

Source: NCBI Gene 2167 — RefSeq curated summary.

At a glance

• Gene–disease (curated): schizophrenia (No Known Disease Relationship, GenCC)
• GWAS associations: 5
• Clinical variants (ClinVar): 16 total
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001442

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3559
Approved symbol	FABP4
Name	fatty acid binding protein 4
Location	8q21.13
Locus type	gene with protein product
Status	Approved
Aliases	A-FABP, aP2
Ensembl gene	ENSG00000170323
Ensembl biotype	protein_coding
OMIM	600434
Entrez	2167

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 5 protein_coding, 1 protein_coding_CDS_not_defined, 1 retained_intron, 1 nonsense_mediated_decay

ENST00000256104, ENST00000518669, ENST00000521734, ENST00000522659, ENST00000956908, ENST00000956909, ENST00000956910, ENST00000956911

RefSeq mRNA: 1 — MANE Select: NM_001442 NM_001442

CCDS: CCDS6230

Canonical transcript exons

ENST00000256104 — 4 exons

Exon	Start	End
ENSE00000795008	81478419	81478915
ENSE00002139695	81483095	81483233
ENSE00003568217	81480426	81480598
ENSE00003684786	81479414	81479515

Expression profiles

Bgee: expression breadth ubiquitous, 238 present calls, max score 99.96.

FANTOM5 (CAGE): breadth broad, TPM avg 429.1988 / max 36484.0712, expressed in 614 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
93762	427.7722	613
93756	0.6480	104
93758	0.4783	103
93757	0.3004	57

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
adipose tissue of abdominal region	UBERON:0007808	99.96	gold quality
omental fat pad	UBERON:0010414	99.95	gold quality
peritoneum	UBERON:0002358	99.89	gold quality
pericardium	UBERON:0002407	99.81	gold quality
adipose tissue	UBERON:0001013	99.78	gold quality
skin of hip	UBERON:0001554	99.75	gold quality
subcutaneous adipose tissue	UBERON:0002190	99.61	gold quality
vena cava	UBERON:0004087	99.57	gold quality
mammary duct	UBERON:0001765	99.45	gold quality
synovial joint	UBERON:0002217	99.43	gold quality
connective tissue	UBERON:0002384	99.38	gold quality
trabecular bone tissue	UBERON:0002483	99.35	gold quality
mucosa of stomach	UBERON:0001199	99.14	gold quality
diaphragm	UBERON:0001103	98.67	gold quality
right lobe of thyroid gland	UBERON:0001119	98.63	gold quality
left lobe of thyroid gland	UBERON:0001120	98.63	gold quality
thoracic mammary gland	UBERON:0005200	98.56	gold quality
mammary gland	UBERON:0001911	98.54	gold quality
right lung	UBERON:0002167	98.53	gold quality
calcaneal tendon	UBERON:0003701	98.53	gold quality
superficial temporal artery	UBERON:0001614	98.43	gold quality
heart right ventricle	UBERON:0002080	98.43	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	98.29	gold quality
thyroid gland	UBERON:0002046	98.28	gold quality
hindlimb stylopod muscle	UBERON:0004252	98.18	gold quality
tibial nerve	UBERON:0001323	98.11	gold quality
gall bladder	UBERON:0002110	98.09	gold quality
cardiac ventricle	UBERON:0002082	98.02	gold quality
heart left ventricle	UBERON:0002084	98.01	gold quality
urinary bladder	UBERON:0001255	97.94	gold quality

Single-cell (SCXA)

Detected in 14 experiment(s), a significant marker in 13.

Experiment	Marker?	Max mean expression
E-MTAB-9841	yes	10817.79
E-HCAD-15	yes	10407.84
E-MTAB-6308	yes	8682.53
E-MTAB-8322	yes	7113.07
E-CURD-126	yes	6190.03
E-MTAB-6653	yes	5105.08
E-HCAD-32	yes	596.22
E-MTAB-8142	yes	41.76
E-GEOD-130148	yes	23.31
E-HCAD-1	yes	21.52
E-CURD-112	yes	13.26
E-MTAB-9067	yes	7.64
E-MTAB-6678	no	3.09
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AEBP1, AEBP2, ASXL1, BMP2, CEBPA, CEBPB, FOXO1, JUN, LRP3, NFE2L2, PPARA, PPARD, PPARG, TFAP2A

miRNA regulators (miRDB)

26 targeting FABP4, 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-4795-3P	100.00	74.62	4024
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-188-3P	100.00	68.76	1240
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-552-5P	99.93	68.56	1583
HSA-MIR-338-5P	99.92	72.34	2951
HSA-MIR-589-3P	99.91	69.62	2088
HSA-MIR-4799-5P	99.82	70.60	2663
HSA-MIR-2681-5P	99.75	67.64	1655
HSA-MIR-561-3P	99.64	70.90	3647
HSA-MIR-12123	99.52	71.79	2990
HSA-MIR-6832-3P	99.52	70.44	1726
HSA-MIR-183-3P	99.41	69.41	1598
HSA-MIR-2115-3P	99.31	69.68	2026
HSA-MIR-499A-3P	99.18	69.20	1392
HSA-MIR-499B-3P	99.18	69.27	1391
HSA-MIR-361-5P	98.95	70.16	1340
HSA-MIR-6878-5P	98.49	67.91	2142
HSA-MIR-2681-3P	98.18	65.28	577
HSA-MIR-188-5P	97.89	67.01	756
HSA-MIR-30C-1-3P	97.80	66.36	1499
HSA-MIR-30C-2-3P	97.80	66.45	1499
HSA-MIR-6788-5P	97.80	66.41	1532
HSA-MIR-6866-3P	97.38	66.94	748
HSA-MIR-4327	97.21	67.71	676
HSA-MIR-5579-5P	96.32	68.54	730

Literature-anchored findings (GeneRIF, showing 40)

• observations suggest that oxLDL-mediated increase in gene expression accelerate cholesterol ester accumulation, and that this is an important component of the genetic program regulating conversion of macrophages to foam cells (PMID:12417276)
• fatty acid binding protein 4 and PPARgamma work together to influence a biologic pathway affecting insulin sensitivity and body composition (PMID:15015141)
• intra-pair correlations revealed that FATP4 expression was signifcantly up-regulated in acquired obesity. (PMID:15168018)
• a pre-lipolysis complex containing at least AFABP and HSL exists (PMID:15456755)
• Loss of expression of A-FABP is associated with progression of bladder carcinoma. (PMID:15734831)
• ALBP gene expression accelerates cholesterol and triglyceride accumulation in macrophage foam cells and affects some key gene expression for lipid metabolism. (PMID:16313911)
• Data demonstrate a significant genetic variation in humans that results in decreased adipose tissue aP2 expression due to alteration of the CAAT box/enhancer-binding protein binding and reduced transcriptional activity of the aP2 promoter. (PMID:16641093)
• FABP4 protein is expressed within the skeletal muscle fibers & FABP4 mRNA & protein are more abundant in the endurance trained subjects.[fatty acid binding protein 4] (PMID:16750515)
• Expression occurs not only in mature adipocytes, but has a wider embryonic expression pattern than previously appreciated. (PMID:16952017)
• the metallothionein genes, adipophilin (ADFP), CD36, adipocyte fatty acid binding protein (FABP4), ATP binding cassette protein A1 (ABCA1), and liver X receptor (LXR[alpha]) all emerged as strongly positively correlated with PPAR[gamma] expression. (PMID:17322100)
• These data indicate for the first time that human macrophage aP2 promoter is a direct target for the regulation by LXR/RXR heterodimers. (PMID:17396233)
• genetic variability at the FABP4 locus has been shown to be associated with plasma lipid levels, type 2 diabetes, and coronary heart disease risk (PMID:17425064)
• There were not significant difference A-FABP expression between ductal infiltrating carcinoma and benign tissue in human breast cancer. (PMID:17428383)
• Changes in DNA methylation at adipogenic promoters during cellular aging. (PMID:17535427)
• thiazolidinedione increases FABP4 plasma concentrations in diabetic patients, reflecting PPARgamma activation (PMID:17553506)
• Hypoxia enhances the expression of FABP4 in term human trophoblasts, suggesting that fatty acid binding proteins support fat accumulation in the hypoxic placenta. (PMID:17826730)
• FABP4 concentrations should be taken into consideration as an early marker of kidney damage in patients with type 2 diabetes. (PMID:18024526)
• human epicardial adipose and ascending aorta tissues express fatty-acid-binding protein 4 and that its level of expression in epicardial adipose tissues of metabolic syndrome patients is elevated (PMID:18417367)
• High FABP4 & low adiponectin levels are independent predictors of atherogenic dyslipidemia. FABP4 plasma concentrations hold strong potential for development as a clinical biomarker for atherogenic dyslipidemia in type 2 diabetic subjects. (PMID:18421072)
• Maternal AFABP serum concentrations are significantly increased in preeclampsia. (PMID:18437151)
• A-FABP serum levels are positively associated with body weight and fat mass (PMID:18535557)
• Serum FABP levels were unchanged in patients with AN and were not related to any of parameters studied (PMID:18657008)
• Exercise training with weight loss induced a significant reduction in circulating A-FABP levels in obese Korean women. (PMID:18710473)
• Mapping of the hormone-sensitive lipase binding site on the adipocyte fatty acid-binding protein (AFABP). Identification of the charge quartet on the AFABP/aP2 helix-turn-helix domain. (PMID:18820256)
• Serum A-FABP is significantly associated with nonalcoholic fatty liver disease in type 2 diabetes, independent of body size, blood lipids and c-reactive protein. (PMID:18835952)
• May be a biomarker for progression of diabetic nephropathy and its cardiovascular risk. (PMID:18931100)
• Serum FABP4 levels increased as the numbers of stenotic coronary artery increased, although these differences were attenuated after adjustment for age and fasting glucose levels (PMID:19001529)
• A-FABP is a candidate progression marker of human transitional cell carcinoma of the bladder that is differentially regulated by PPAR in urothelial cancer cells (PMID:19115207)
• Adipocyte-fatty acid binding protein may play a role in obstructive sleep apnoea and metabolic dysfunction (PMID:19181913)
• Examine adipocyte fatty acid-binding protein as a determinant of insulin sensitivity in morbid-obese women. (PMID:19197257)
• Serum A-FABP concentrations were significantly correlated with BMI and waist circumference (PMID:19368945)
• results indicate that variation in A-FABP plasma levels reflect alterations in nutritional status in patients with anorexia nervosa (PMID:19421706)
• Increased circulating AFABP and RBP-4 concentrations were demonstrated in patients with preeclampsia, suggesting it be an important pathophysiology of preeclampsia. (PMID:19573524)
• the release of FABP4 from adipocytes may be involved in the development of cardiac contractile dysfunction of obese subjects. (PMID:19608978)
• FABP4 emerged as a novel target of the VEGF/VEGFR2 pathway and a positive regulator of cell proliferation in endothelial cells. (PMID:19625659)
• Study reveals that high A-FABP serum levels are associated with obesity, breast cancer risk, and adverse tumor characteristics. (PMID:19842034)
• An association between FABP4 gene polymorphisms and the development of polycystic ovary syndrome. (PMID:19844814)
• Interaction between PTEN to FABP4 suggests a role for this phosphatase in the regulation of lipid metabolism and adipocyte differentiation. (PMID:19911253)
• Among coronary artery disease patients the fasting level of FABP4 positively correlated with metabolic syndrome and serum levels of FABP4 correlated with a number of MetS criteria. (PMID:20009357)
• our finding from a multiethnic cohort of postmenopausal women did not support the notion that common genetic variants in the FABP4 gene may trigger increased risk of type 2 diabetes mellitus (PMID:20111020)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	rbp7a	ENSDARG00000091906
danio_rerio	rbp5	ENSDARG00000101481
mus_musculus	Fabp4	ENSMUSG00000062515
rattus_norvegicus	Fabp4	ENSRNOG00000010805
drosophila_melanogaster	fabp	FBGN0037913
caenorhabditis_elegans		WBGENE00021486

Paralogs (15): RBP2 (ENSG00000114113), RBP1 (ENSG00000114115), FABP3 (ENSG00000121769), RBP5 (ENSG00000139194), CRABP2 (ENSG00000143320), FABP2 (ENSG00000145384), PMP2 (ENSG00000147588), RBP7 (ENSG00000162444), FABP1 (ENSG00000163586), FABP7 (ENSG00000164434), FABP5 (ENSG00000164687), CRABP1 (ENSG00000166426), FABP6 (ENSG00000170231), FABP12 (ENSG00000197416), FABP9 (ENSG00000205186)

Protein

Protein identifiers

Fatty acid-binding protein, adipocyte — P15090 (reviewed: P15090)

Alternative names: Adipocyte lipid-binding protein, Adipocyte-type fatty acid-binding protein, Fatty acid-binding protein 4

All UniProt accessions (3): P15090, E5RIR0, E7DVW4

UniProt curated annotations — full annotation on UniProt →

Function. Lipid transport protein in adipocytes. Binds both long chain fatty acids and retinoic acid. Delivers long-chain fatty acids and retinoic acid to their cognate receptors in the nucleus.

Subunit / interactions. Monomer. Homodimer. Interacts with PPARG.

Subcellular location. Cytoplasm. Nucleus.

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

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

RefSeq proteins (1): NP_001433* (*=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

UniProt features (22 total): strand 11, helix 3, modified residue 3, initiator methionine 1, chain 1, short sequence motif 1, binding site 1, sequence variant 1

Structure

Experimental structures (PDB)

248 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
7G0Z	X-RAY DIFFRACTION	0.84
7FXV	X-RAY DIFFRACTION	0.88
7G1F	X-RAY DIFFRACTION	0.91
7G1R	X-RAY DIFFRACTION	0.93
7FYG	X-RAY DIFFRACTION	0.94
7FWK	X-RAY DIFFRACTION	0.95
7FXF	X-RAY DIFFRACTION	0.95
7G05	X-RAY DIFFRACTION	0.95
7G1Y	X-RAY DIFFRACTION	0.95
7FZ9	X-RAY DIFFRACTION	0.96
7FYV	X-RAY DIFFRACTION	0.97
7G1L	X-RAY DIFFRACTION	0.98
7FX1	X-RAY DIFFRACTION	0.99
7FXR	X-RAY DIFFRACTION	0.99
7FZ1	X-RAY DIFFRACTION	0.99
7FZO	X-RAY DIFFRACTION	0.99
7G08	X-RAY DIFFRACTION	0.99
7G0Y	X-RAY DIFFRACTION	0.99
7FVY	X-RAY DIFFRACTION	1
7FW9	X-RAY DIFFRACTION	1
7FWU	X-RAY DIFFRACTION	1.01
7FZ4	X-RAY DIFFRACTION	1.01
7FX4	X-RAY DIFFRACTION	1.02
7FXH	X-RAY DIFFRACTION	1.02
7FXN	X-RAY DIFFRACTION	1.02
7FYF	X-RAY DIFFRACTION	1.02
7FZ0	X-RAY DIFFRACTION	1.02
7FZD	X-RAY DIFFRACTION	1.02
7G0P	X-RAY DIFFRACTION	1.02
7G0Q	X-RAY DIFFRACTION	1.02

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P15090-F1	95.90	0.95

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 (1): 127–129

Post-translational modifications (3): 2, 13, 20

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-163560	Triglyceride catabolism
R-HSA-381340	Transcriptional regulation of white adipocyte differentiation
R-HSA-9841922	MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis

MSigDB gene sets: 342 (showing top): GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_UP, REACTOME_TRIGLYCERIDE_CATABOLISM, REACTOME_TRANSCRIPTIONAL_REGULATION_OF_WHITE_ADIPOCYTE_DIFFERENTIATION, MODULE_52, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, HNF3ALPHA_Q6, GOBP_INFLAMMATORY_RESPONSE, GOBP_RESPONSE_TO_PEPTIDE, GOBP_STEROL_HOMEOSTASIS, GOBP_WHITE_FAT_CELL_DIFFERENTIATION, SMID_BREAST_CANCER_RELAPSE_IN_LUNG_DN, DARWICHE_SKIN_TUMOR_PROMOTER_UP, DARWICHE_PAPILLOMA_RISK_LOW_UP, DARWICHE_PAPILLOMA_RISK_HIGH_UP, DARWICHE_SQUAMOUS_CELL_CARCINOMA_UP

GO Biological Process (12): response to bacterium (GO:0009617), fatty acid transport (GO:0015908), long-chain fatty acid transport (GO:0015909), cholesterol homeostasis (GO:0042632), negative regulation of DNA-templated transcription (GO:0045892), positive regulation of inflammatory response (GO:0050729), white fat cell differentiation (GO:0050872), brown fat cell differentiation (GO:0050873), white fat cell proliferation (GO:0070343), cellular response to lithium ion (GO:0071285), cellular response to tumor necrosis factor (GO:0071356), positive regulation of cold-induced thermogenesis (GO:0120162)

GO Molecular Function (5): long-chain fatty acid transmembrane transporter activity (GO:0005324), fatty acid binding (GO:0005504), long-chain fatty acid binding (GO:0036041), hormone receptor binding (GO:0051427), lipid binding (GO:0008289)

GO Cellular Component (5): nucleus (GO:0005634), cytoplasm (GO:0005737), lipid droplet (GO:0005811), cytosol (GO:0005829), extracellular exosome (GO:0070062)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Triglyceride metabolism	1
Adipogenesis	1
Epigenetic regulation of adipogenesis genes by MLL3 and MLL4 complexes	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
fat cell differentiation	2
cellular anatomical structure	2
response to other organism	1
lipid transport	1
monocarboxylic acid transport	1
fatty acid transport	1
sterol homeostasis	1
DNA-templated transcription	1
regulation of DNA-templated transcription	1
negative regulation of RNA biosynthetic process	1
inflammatory response	1
positive regulation of defense response	1
positive regulation of response to external stimulus	1
regulation of inflammatory response	1
fat cell proliferation	1
response to lithium ion	1
cellular response to metal ion	1
response to tumor necrosis factor	1
cellular response to cytokine stimulus	1
positive regulation of multicellular organismal process	1
cold-induced thermogenesis	1
regulation of cold-induced thermogenesis	1
fatty acid transmembrane transporter activity	1
long-chain fatty acid transport	1
lipid binding	1
monocarboxylic acid binding	1
fatty acid binding	1
signaling receptor binding	1
binding	1
intracellular membrane-bounded organelle	1
intracellular anatomical structure	1
intracellular membraneless organelle	1
cytoplasm	1
extracellular vesicle	1

Protein interactions and networks

STRING

2508 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FABP4	LIPE	Q05469	994
FABP4	PPARG	P37231	983
FABP4	GOT2	P00505	897
FABP4	LPL	P06858	882
FABP4	CD36	P16671	881
FABP4	SCARB2	Q14108	865
FABP4	SCARB1	Q8WTV0	864
FABP4	ADIPOQ	Q15848	842
FABP4	CEBPA	P49715	829
FABP4	FABP1	P07148	816
FABP4	SREBF1	P36956	799
FABP4	PPARA	Q07869	790
FABP4	DGAT2	Q96PD7	782
FABP4	PLIN1	O60240	774
FABP4	LEP	P41159	763

IntAct

23 interactions, top by confidence:

A	B	Type	Score
OAZ3	AZIN1	psi-mi:“MI:0914”(association)	0.800
VIM	FABP4	psi-mi:“MI:0915”(physical association)	0.550
GDF5	SERPINB7	psi-mi:“MI:0914”(association)	0.530
VPS35	SPAG9	psi-mi:“MI:0914”(association)	0.530
FABP4	ZNF16	psi-mi:“MI:0915”(physical association)	0.370
ACTB	FABP4	psi-mi:“MI:0915”(physical association)	0.370
CHD3	FABP4	psi-mi:“MI:0915”(physical association)	0.370
FABP4	PRKCI	psi-mi:“MI:0915”(physical association)	0.370
FABP4	ZBED1	psi-mi:“MI:0915”(physical association)	0.370
FABP4	TFAP2C	psi-mi:“MI:0915”(physical association)	0.370
USP15	KRT35	psi-mi:“MI:0914”(association)	0.350
FOXN3	IGLL5	psi-mi:“MI:0914”(association)	0.350
VIPR2	EI24	psi-mi:“MI:0914”(association)	0.350
SCG5	MACROH2A1	psi-mi:“MI:0914”(association)	0.350
S1PR4	ECD	psi-mi:“MI:0914”(association)	0.350
CDH5	ESYT2	psi-mi:“MI:2364”(proximity)	0.270
FABP4	SNCG	psi-mi:“MI:0915”(physical association)	0.000
FABP4	OSTF1	psi-mi:“MI:0915”(physical association)	0.000
FABP4	EXT2	psi-mi:“MI:0915”(physical association)	0.000
FABP4	VIM	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (38): LIPE (FRET), FABP4 (FRET), FABP4 (Affinity Capture-MS), FABP4 (Affinity Capture-MS), OSTF1 (Affinity Capture-MS), SNCG (Affinity Capture-MS), EXT2 (Affinity Capture-MS), FABP4 (Negative Genetic), FABP4 (Negative Genetic), SLC16A8 (Negative Genetic), PTGIR (Negative Genetic), FABP4 (Negative Genetic), FABP4 (Negative Genetic), MST1R (Negative Genetic), PIK3C2B (Negative Genetic)

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

4 interactions.

A	Effect	B	Mechanism
FABP4	“up-regulates quantity”	“Fatty acid”	relocalization
PPARG	“up-regulates quantity by expression”	FABP4	“transcriptional regulation”
PPARG	up-regulates	FABP4	“transcriptional regulation”
INSR	unknown	FABP4	phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	10
Likely benign	2
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

262 predictions. Top by Δscore:

Variant	Effect	Δscore
8:81478913:TTC:T	acceptor_gain	1.0000
8:81478916:C:CC	acceptor_gain	1.0000
8:81479405:GATAC:G	donor_loss	1.0000
8:81479406:ATAC:A	donor_loss	1.0000
8:81479407:TACT:T	donor_loss	1.0000
8:81479408:AC:A	donor_loss	1.0000
8:81479409:CT:C	donor_loss	1.0000
8:81479410:T:TA	donor_loss	1.0000
8:81479411:CA:C	donor_loss	1.0000
8:81479413:C:CT	donor_loss	1.0000
8:81479514:CT:C	acceptor_gain	1.0000
8:81479516:C:CC	acceptor_gain	1.0000
8:81480412:T:TA	donor_gain	1.0000
8:81480421:CTCA:C	donor_loss	1.0000
8:81480422:TCA:T	donor_loss	1.0000
8:81480423:CA:C	donor_loss	1.0000
8:81480424:A:C	donor_loss	1.0000
8:81480425:CCTT:C	donor_loss	1.0000
8:81480434:T:A	donor_gain	1.0000
8:81480596:CTC:C	acceptor_gain	1.0000
8:81480597:TCC:T	acceptor_loss	1.0000
8:81480599:C:CG	acceptor_loss	1.0000
8:81480605:T:TC	acceptor_gain	1.0000
8:81483094:CCTA:C	donor_gain	1.0000
8:81483097:A:AC	donor_gain	1.0000
8:81483098:C:CC	donor_gain	1.0000
8:81478911:CATTC:C	acceptor_gain	0.9900
8:81478915:CCTA:C	acceptor_loss	0.9900
8:81478916:C:CA	acceptor_loss	0.9900
8:81478917:T:G	acceptor_loss	0.9900

AlphaMissense

879 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
8:81480435:C:A	R79S	0.996
8:81480435:C:G	R79S	0.996
8:81480571:G:T	A34D	0.996
8:81480579:C:A	R31S	0.995
8:81480579:C:G	R31S	0.995
8:81479513:G:C	S83R	0.994
8:81479513:G:T	S83R	0.994
8:81479515:T:G	S83R	0.994
8:81480580:C:G	R31T	0.993
8:81483143:A:G	W9R	0.993
8:81483143:A:T	W9R	0.993
8:81479441:T:A	R107S	0.992
8:81479441:T:G	R107S	0.992
8:81480504:A:C	S56R	0.992
8:81480504:A:T	S56R	0.992
8:81480506:T:G	S56R	0.992
8:81483117:A:C	F17L	0.992
8:81483117:A:T	F17L	0.992
8:81483119:A:G	F17L	0.992
8:81480436:C:A	R79M	0.991
8:81480580:C:A	R31M	0.991
8:81483141:C:A	W9C	0.991
8:81483141:C:G	W9C	0.991
8:81479508:A:T	I85K	0.990
8:81480436:C:G	R79T	0.990
8:81478891:A:G	S125P	0.989
8:81480443:C:G	D77H	0.989
8:81480459:A:C	F71L	0.989
8:81480459:A:T	F71L	0.989
8:81480461:A:G	F71L	0.989

dbSNP variants (sampled 300 via entrez): RS1000773487 (8:81483003 G>A,C), RS1000985765 (8:81483545 G>A,C), RS1001941666 (8:81483555 T>C), RS1002255934 (8:81481648 G>A), RS1002714713 (8:81482066 T>C), RS1002728692 (8:81480044 C>T), RS1003231434 (8:81480320 G>A), RS1003610585 (8:81484768 T>C), RS1003662947 (8:81484929 C>G,T), RS1004012202 (8:81480994 G>A), RS1006095705 (8:81482604 T>C), RS1006163480 (8:81479146 C>T), RS1006215845 (8:81479407 TACTC>T), RS1006545772 (8:81478137 C>T), RS1006804362 (8:81482916 G>C)

Disease associations

OMIM: gene MIM:600434 | disease phenotypes:

GenCC curated gene-disease

Disease	Classification	Inheritance
schizophrenia	No Known Disease Relationship	Unknown

Mondo (1): schizophrenia (MONDO:0005090)

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST001525_37	Visceral fat	7.000000e-07
GCST001941_13	Ovarian cancer	6.000000e-09
GCST001941_17	Ovarian cancer	7.000000e-10
GCST006585_2476	Blood protein levels	7.000000e-07
GCST009391_513	Metabolite levels	2.000000e-07

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0010117	pyruvate measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2083 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,050,204 (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
CHEMBL186141	ANDROGRAPHOLIDE	3	404
CHEMBL267476	LINOLEIC ACID	2	323,195
CHEMBL8659	OLEIC ACID	2	713,838
CHEMBL23832	FENAMIC ACID	1	12,767

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 (4 total), top 4:

Ligand	Action	Affinity	Parameter
HM50316	Inhibition	9.0	pKi
compound 13 [PMID: 17502136]	Inhibition	8.7	pKi
HTS01037	Inhibition	6.17	pKi
bindarit	Binding	4.72	pKi

Binding affinities (BindingDB)

309 measured of 358 human assays (358 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
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
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
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
2-[[4-cyclopropyl-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)thiophen-2-yl]carbamoyl]cyclopentene-1-carboxylic acid	IC50	38.8 nM	US-9353102: Non-annulated thiophenylamides
2-[[5-cyclopropyl-4-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)thiophen-2-yl]carbamoyl]cyclohexene-1-carboxylic acid	IC50	39 nM	US-9353102: Non-annulated thiophenylamides
3-[[(6S)-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	39 nM	US-9604977: Bicyclic thiophenylamide compounds

ChEMBL bioactivities

696 potent at pChembl≥5 of 756 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.00	Ki	0.1	nM	CHEMBL5272139
8.70	Ki	2	nM	CHEMBL247298
8.60	Ki	2.5	nM	CHEMBL378857
8.57	Ki	2.7	nM	CHEMBL245282
8.48	Ki	3.3	nM	CHEMBL245284
8.47	Ki	3.4	nM	CHEMBL245653
8.46	Ki	3.5	nM	CHEMBL247529
8.40	Kd	4	nM	CHEMBL247920
8.30	Ki	5	nM	CHEMBL1782966
8.22	Ki	6	nM	CHEMBL126078
8.22	Ki	6	nM	CHEMBL1782968
8.15	Ki	7	nM	CHEMBL3970105
8.15	Ki	7	nM	CHEMBL1782965
8.13	Ki	7.4	nM	CHEMBL247920
8.06	Ki	8.7	nM	CHEMBL397385
8.05	IC50	9	nM	CHEMBL5987465
8.03	Ki	9.3	nM	CHEMBL248144
8.00	IC50	10	nM	CHEMBL3918729
8.00	IC50	10	nM	CHEMBL3919426
8.00	IC50	10	nM	CHEMBL3896829
8.00	IC50	10	nM	CHEMBL3905766
8.00	Kd	10	nM	CHEMBL4581404
8.00	IC50	10	nM	CHEMBL5278127
8.00	IC50	10	nM	CHEMBL5281007
8.00	Kd	10	nM	CHEMBL4560388
8.00	IC50	10	nM	CHEMBL6040071
8.00	IC50	10	nM	CHEMBL5912944
8.00	IC50	10	nM	CHEMBL5745897
8.00	IC50	10	nM	CHEMBL5916833
8.00	IC50	10	nM	CHEMBL5894731
8.00	IC50	10	nM	CHEMBL5929433
8.00	IC50	10	nM	CHEMBL5992918
8.00	IC50	10	nM	CHEMBL5743635
8.00	IC50	10	nM	CHEMBL5872270
8.00	IC50	10	nM	CHEMBL5957946
8.00	IC50	10	nM	CHEMBL6023976
7.96	Ki	11	nM	CHEMBL3959018
7.96	IC50	11	nM	CHEMBL3915309
7.96	IC50	11	nM	CHEMBL5968058
7.92	Ki	12	nM	CHEMBL3947458
7.92	Ki	12	nM	CHEMBL394966
7.92	IC50	12	nM	CHEMBL6052767
7.92	IC50	12	nM	CHEMBL5990195
7.89	Ki	13	nM	CHEMBL3950316
7.89	IC50	13	nM	CHEMBL3914116
7.89	IC50	13	nM	CHEMBL3923099
7.89	Ki	13	nM	CHEMBL245653
7.89	Ki	13	nM	CHEMBL396698
7.89	IC50	13	nM	CHEMBL5268623
7.89	IC50	13	nM	CHEMBL5268944

PubChem BioAssay actives

389 with measured affinity, of 794 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
8-chloro-3-[2-[(3,5-dichlorophenyl)methyl]pyrrolidine-1-carbonyl]-1H-quinoxalin-2-one	1958769: Binding affinity to FABP4 (unknown origin) assessed as inhibition constant	ki	0.0001	uM
2-[3-[2-[1-(4-chlorophenyl)-5-thiophen-2-ylpyrazol-3-yl]phenyl]phenoxy]propanoic acid	601694: Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry	ki	0.0010	uM
2-[3-[2-[1-(4-chlorophenyl)-5-thiophen-2-ylpyrazol-3-yl]phenyl]phenoxy]-2-methylpropanoic acid	601694: Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry	ki	0.0010	uM
2-[3-[2-(1-ethyl-4,5-diphenylimidazol-2-yl)phenyl]phenoxy]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0020	uM
2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetic acid	1958759: Inhibition of human FABP4 assessed as inhibition constant by fluorescent displacement assay	ki	0.0020	uM
2-[3-[2-(1-methyl-4,5-diphenylimidazol-2-yl)phenyl]phenoxy]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0020	uM
2-[3-[2-[1-(2-fluoroethyl)-4,5-diphenylimidazol-2-yl]phenyl]phenoxy]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0020	uM
2-[2,3-bis[(2-chlorophenyl)methoxy]phenyl]-2-oxoacetic acid	268958: Binding affinity to ap2	ki	0.0020	uM
2,3-bis[(2,4-dichloro-3-tritiophenyl)methoxy]benzoic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0020	uM
(2S)-2-[2,3-bis[(2-chlorophenyl)methoxy]phenyl]-2-hydroxyacetic acid	268958: Binding affinity to ap2	ki	0.0025	uM
2-[3-[2-(1-methyl-4,5-diphenylimidazol-2-yl)phenyl]anilino]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0027	uM
2-[3-[2-(1-ethyl-4,5-diphenylimidazol-2-yl)phenyl]anilino]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0034	uM
2-[3-[2-(3-ethyl-4,5-diphenylfuran-2-yl)phenyl]phenoxy]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0035	uM
2-[3-[2-[1-(4-chlorophenyl)-5-thiophen-2-ylpyrazol-3-yl]phenyl]phenoxy]acetic acid	601694: Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry	ki	0.0050	uM
2-[3-[2-[1-(4-chlorophenyl)-5-thiophen-2-ylpyrazol-3-yl]phenyl]phenoxy]butanoic acid	601694: Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry	ki	0.0060	uM
2-[3-[2-(4,5-diphenyl-1,3-oxazol-2-yl)phenyl]phenoxy]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0060	uM
2-[3-[2-[1-(4-chlorophenyl)-5-(furan-2-yl)pyrazol-3-yl]phenyl]phenoxy]acetic acid	601694: Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry	ki	0.0070	uM
5-(6-chloro-4-phenyl-2-piperidin-1-ylquinolin-3-yl)-3H-1,3,4-oxadiazole-2-thione	1322079: Displacement of Bodipy-labeled fatty acid from recombinant human His6-tagged FABP4 expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.0070	uM
2-[3-[2-(4,5-diphenyl-1H-imidazol-2-yl)phenyl]phenoxy]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0093	uM
5-[(3-chloro-2-methylanilino)methyl]-2-phenyl-1H-[1,2,4]triazolo[1,5-a]pyrimidin-7-one	1638396: Binding affinity to recombinant FABP4 (unknown origin) expressed in Escherichia coli by sypro orange dye-based TdF assay	kd	0.0100	uM
5-[(3-chloro-2-methylphenoxy)methyl]-2-phenyl-1H-[1,2,4]triazolo[1,5-a]pyrimidin-7-one	1958771: Binding affinity to human FABP4 expressed in Escherichia coli assessed as degree of fluorescent shift by temperature-dependent fluorescence thermal shift assay	kd	0.0100	uM
2-cyclopentyl-6-methyl-4-(2-methyl-4-pyridinyl)-3-(2H-tetrazol-5-yl)-5,6,7,8-tetrahydroquinoline	1958766: Inhibition of human FABP4	ic50	0.0100	uM
2-(1-methylcyclopentyl)-4-(2-methyl-4-pyridinyl)-3-(2H-tetrazol-5-yl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine	1958766: Inhibition of human FABP4	ic50	0.0100	uM
6-chloro-4-phenyl-2-piperidin-1-yl-3-(2H-tetrazol-5-yl)quinoline	1322079: Displacement of Bodipy-labeled fatty acid from recombinant human His6-tagged FABP4 expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.0110	uM
6-chloro-4-phenyl-2-propan-2-ylquinoline-3-carboxylic acid	1322079: Displacement of Bodipy-labeled fatty acid from recombinant human His6-tagged FABP4 expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.0120	uM
2-[3-[2-(4,5-diphenyl-1H-pyrrol-2-yl)phenyl]phenoxy]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0120	uM
2-[3-[2-[1-(4-chlorophenyl)-5-phenylpyrazol-3-yl]phenyl]phenoxy]acetic acid	601694: Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry	ki	0.0130	uM
6-chloro-8-methyl-4-phenyl-2-piperidin-1-ylquinoline-3-carboxylic acid	1322079: Displacement of Bodipy-labeled fatty acid from recombinant human His6-tagged FABP4 expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.0130	uM
6-chloro-7-fluoro-4-phenyl-2-piperidin-1-yl-3-(2H-tetrazol-5-yl)quinoline	1958760: Inhibition of FABP4 (unknown origin)	ic50	0.0130	uM
6-chloro-N,N-diethyl-7-fluoro-4-phenyl-3-(2H-tetrazol-5-yl)quinolin-2-amine	1958760: Inhibition of FABP4 (unknown origin)	ic50	0.0130	uM
2-[2,3-bis[(2-chlorophenyl)methoxy]phenyl]acetic acid	268958: Binding affinity to ap2	ki	0.0160	uM
6,8-dichloro-4-phenyl-2-piperidin-1-ylquinoline-3-carboxylic acid	1322079: Displacement of Bodipy-labeled fatty acid from recombinant human His6-tagged FABP4 expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.0160	uM
6-chloro-2-(dimethylamino)-4-(3-propan-2-ylphenyl)quinoline-3-carboxylic acid	1322079: Displacement of Bodipy-labeled fatty acid from recombinant human His6-tagged FABP4 expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.0160	uM
6-chloro-7-fluoro-2-pentan-3-yl-4-phenyl-3-(2H-tetrazol-5-yl)quinoline	1958760: Inhibition of FABP4 (unknown origin)	ic50	0.0170	uM
2-[3-[2-(4,5-diphenyl-1H-imidazol-2-yl)phenyl]anilino]acetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0180	uM
2-chloro-6-(3-chloro-2-phenylanilino)benzoic acid	2096492: Binding affinity to N-terminal 6His-tagged full length FABP4 (unknown origin) expressed in Escherichia coli ER2566 assessed as dissociation constant by isothermal titration calorimetric analysis	kd	0.0190	uM
2-[1-(methoxymethyl)cyclopentyl]-6-pentyl-4-phenyl-3-(2H-tetrazol-5-yl)-5,6,7,8-tetrahydroquinoline	1958766: Inhibition of human FABP4	ic50	0.0200	uM
5-[(3-chloro-2-cyclopropylanilino)methyl]-2-phenyl-1H-[1,2,4]triazolo[1,5-a]pyrimidin-7-one	1638396: Binding affinity to recombinant FABP4 (unknown origin) expressed in Escherichia coli by sypro orange dye-based TdF assay	kd	0.0200	uM
6-chloro-5-[(3-chloro-2-cyclopropylphenoxy)methyl]-2-phenyl-1H-[1,2,4]triazolo[1,5-a]pyrimidin-7-one	1958771: Binding affinity to human FABP4 expressed in Escherichia coli assessed as degree of fluorescent shift by temperature-dependent fluorescence thermal shift assay	kd	0.0200	uM
5-(6-chloro-4-phenyl-2-piperidin-1-ylquinolin-3-yl)-3H-1,3,4-oxadiazol-2-one	1322079: Displacement of Bodipy-labeled fatty acid from recombinant human His6-tagged FABP4 expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	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	1958766: Inhibition of human FABP4	ic50	0.0200	uM
6-chloro-4-phenyl-2-piperidin-1-ylquinoline-3-carboxylic acid	1322079: Displacement of Bodipy-labeled fatty acid from recombinant human His6-tagged FABP4 expressed in Escherichia coli after 30 mins by TR-FRET assay	ki	0.0220	uM
2-(3-chloro-2-phenylanilino)-6-methylbenzoic acid	2096492: Binding affinity to N-terminal 6His-tagged full length FABP4 (unknown origin) expressed in Escherichia coli ER2566 assessed as dissociation constant by isothermal titration calorimetric analysis	kd	0.0250	uM
N,N-diethyl-4-phenyl-3-(2H-tetrazol-5-yl)-6-(trifluoromethyl)quinolin-2-amine	1958760: Inhibition of FABP4 (unknown origin)	ic50	0.0250	uM
2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenyl]-2-hydroxyacetic acid	307907: Displacement of 1,8-ANS from aFABP by fluorescence based-assay	ki	0.0280	uM
3-[5-cyclopropyl-3-(3,5-dimethyl-1H-pyrazol-4-yl)-2-(3-propan-2-yloxyphenyl)indol-1-yl]propanoic acid	1305257: Binding affinity to His-tagged human recombinant FABP4 expressed in Escherichia coli BL21 (DE3) by fluorescence assay	ki	0.0300	uM
6-chloro-2-ethyl-4-phenylquinoline-3-carboxylic acid	1949363: Inhibition of FABP4 (unknown origin) assessed as inhibition constant	ki	0.0300	uM
2-[3-[2-(1,5-diphenylpyrazol-3-yl)phenyl]phenoxy]acetic acid	601694: Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry	ki	0.0320	uM
4-phenyl-2-piperidin-1-yl-3-(2H-tetrazol-5-yl)-6-(trifluoromethyl)quinoline	1958760: Inhibition of FABP4 (unknown origin)	ic50	0.0330	uM
2-(3-chloro-2-phenylanilino)benzoic acid	1648407: Binding affinity at recombinant human 6His-tagged FABP4 expressed in Escherichia coli BL21 DE3 by isothermal titration calorimetry	kd	0.0344	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Rosiglitazone	affects cotreatment, increases expression, decreases reaction, affects reaction	21
Dexamethasone	increases reaction, affects response to substance, decreases expression, affects expression, affects cotreatment (+2 more)	20
1-Methyl-3-isobutylxanthine	increases reaction, affects response to substance, decreases expression, affects expression, affects cotreatment (+2 more)	17
bisphenol A	affects cotreatment, increases expression, decreases expression, decreases reaction, affects reaction	10
bisphenol S	increases expression, decreases expression, decreases reaction, affects reaction, affects cotreatment	8
Troglitazone	increases expression, decreases reaction, affects cotreatment	7
sodium arsenite	decreases expression, increases abundance, increases expression	5
Indomethacin	affects response to substance, decreases expression, decreases reaction, increases expression, affects cotreatment	5
Valproic Acid	decreases methylation, increases expression, increases reaction, decreases expression	4
bisphenol F	affects expression, affects cotreatment, increases expression	3
2-chloro-5-nitrobenzanilide	affects cotreatment, decreases reaction, increases expression	3
T 0070907	affects cotreatment, decreases expression, decreases reaction, increases expression	3
Pioglitazone	affects cotreatment, increases expression	3
Tetrachlorodibenzodioxin	decreases expression, affects expression	3
Mifepristone	affects cotreatment, increases expression, decreases reaction	3
Firemaster 550	affects cotreatment, increases expression	2
oxybenzone	affects cotreatment, increases expression, increases reaction	2
triphenyl phosphate	affects cotreatment, increases expression, decreases reaction	2
tributyltin	decreases reaction, increases expression	2
3,4,5,3’,4’-pentachlorobiphenyl	decreases expression	2
sulindac sulfide	decreases reaction, increases expression, affects reaction	2
avobenzone	affects cotreatment, increases expression, increases reaction	2
perfluorooctane sulfonic acid	increases expression	2
2-(2’-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)biphenyl-3-yloxy)acetic acid	decreases reaction, increases expression	2
bisphenol AF	increases expression, affects cotreatment	2
Resveratrol	affects secretion, decreases expression	2
Fulvestrant	decreases reaction, increases expression	2
Arsenic	affects methylation, decreases expression, increases abundance	2
Berberine	increases expression, increases reaction, decreases expression	2
Ibuprofen	decreases expression, increases expression	2

ChEMBL screening assays

73 unique, capped per target: 73 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1100873	Binding	Binding affinity to AFABP in forskolin-stimulated human C8PA cells assessed as blocked of protein interaction with hormone sensitive lipase at 1 uM after 2 to 4 hrs by FRET analysis	Identification and characterization of a small molecule inhibitor of Fatty Acid binding proteins. — J Med Chem

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B7X9	Abcam Raji FABP4 KO	Cancer cell line	Male
CVCL_B9XW	Abcam THP-1 FABP4 KO	Cancer cell line	Male
CVCL_C6ZR	Abcam PC-3 FABP4 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00000374	PHASE4	COMPLETED	Treatment for First-Episode Schizophrenia
NCT00001656	PHASE4	COMPLETED	Comparison of Clozapine vs Olanzapine in Childhood-Onset Psychotic Disorders
NCT00007774	PHASE4	COMPLETED	To Determine if Olanzapine is More Cost Effective Than Haloperidol for the Treatment of Schizophrenia
NCT00014001	PHASE4	COMPLETED	CATIE- Schizophrenia Trial
NCT00018668	PHASE4	COMPLETED	Antipsychotic Response in Schizophrenia
NCT00034801	PHASE4	COMPLETED	Olanzapine Versus Active Comparator in the Treatment of Depression in Patients With Schizophrenia
NCT00034905	PHASE4	COMPLETED	A Comparison of Seroquel vs. Risperidone in Schizophrenia
NCT00036088	PHASE4	COMPLETED	Olanzapine Versus An Active Comparator in the Treatment of Schizophrenia
NCT00044187	PHASE4	COMPLETED	The Assessment of a Weight-Gain Agent for the Treatment of Olanzapine-Associated Anti-Obesity Agent in Patients With Schizophrenia, Schizophreniform Disorder, Schizoaffective Disorder, and Bipolar I Disorder
NCT00044655	PHASE4	COMPLETED	Switching Medication to Treat Schizophrenia
NCT00048828	PHASE4	COMPLETED	Treating Drug-Resistant Childhood Schizophrenia
NCT00053703	PHASE4	COMPLETED	Treatment of Early Onset Schizophrenia Spectrum Disorders (TEOSS)
NCT00056498	PHASE4	COMPLETED	Risperidone Treatment in Schizophrenia Patients Who Are Currently Taking Clozapine
NCT00061802	PHASE4	COMPLETED	Efficacy and Safety of Two Atypical Antipsychotics vs. Placebo in Patients With an Acute Exacerbation of Either Schizophrenia or Schizoaffective Disorder
NCT00080327	PHASE4	COMPLETED	Study of Three Doses of Aripiprazole in Patients With Acute Schizophrenia
NCT00088049	PHASE4	COMPLETED	Study of Olanzapine vs. Aripiprazole in the Treatment of Schizophrenia
NCT00090012	PHASE4	COMPLETED	Comparison of Continuing Olanzapine to Switching to Quetiapine in Overweight or Obese Patients With Schizophrenia and Schizoaffective Disorder
NCT00100776	PHASE4	COMPLETED	Efficacy of High Dose Olanzapine for the Treatment of Schizophrenia and Schizoaffective Disorder
NCT00103571	PHASE4	COMPLETED	Olanzapine Versus Aripiprazole in the Treatment of Acutely Ill Patients With Schizophrenia
NCT00108368	PHASE4	COMPLETED	The Effects of Risperidone and Olanzapine on Thinking
NCT00114595	PHASE4	COMPLETED	Ethyl-Eicosapentaenoic Acid and Tardive Dyskinesia
NCT00130923	PHASE4	COMPLETED	Risperidone Long-acting Versus Oral Risperidone in Patients With Schizophrenia and Alcohol Use Disorder
NCT00137020	PHASE4	COMPLETED	Clinical Effect Of Cross Titration Of Antipsychotics With Ziprasidone In Schizophrenia Or Schizoaffective Disorder
NCT00140166	PHASE4	COMPLETED	Treatment of Acute Schizophrenia With Vitamin Therapy
NCT00145847	PHASE4	COMPLETED	Naltrexone Treatment of Alcohol Abuse in Schizophrenia
NCT00148564	PHASE4	COMPLETED	Energy Homeostasis Under Treatment With Atypical Antipsychotics
NCT00156715	PHASE4	COMPLETED	Efficacy of Quetiapine in the Treatment of Patients With Schizophrenia and a Comorbid Substance Use Disorder
NCT00158223	PHASE4	COMPLETED	Effectiveness of Pimozide in Augmenting the Effects of Clozapine in the Treatment of Schizophrenia
NCT00159081	PHASE4	COMPLETED	One Year Drug Treatment in First-Episode Schizophrenia
NCT00159120	PHASE4	COMPLETED	Maintenance Treatment vs. Stepwise Drug Discontinuation in First-Episode Schizophrenia
NCT00159133	PHASE4	COMPLETED	Prodrome-Based Early Intervention With Antipsychotics vs. Benzodiazepines in First-Episode Schizophrenia
NCT00159757	PHASE4	TERMINATED	12 Week Open, Non-Comparative Switch Study Of Oral Ziprazidone In Previously Treated Schizophrenic Patients
NCT00167817	PHASE4	COMPLETED	Effect of Switch to Aripiprazole on Health and Smoking Parameters in Patients With Schizophrenia: A Pilot Study
NCT00169026	PHASE4	TERMINATED	Alcoholism and Schizophrenia: Effects of Clozapine
NCT00169039	PHASE4	TERMINATED	Clozapine Versus Chlorpromazine for Treatment-Unresponsive Schizophrenia
NCT00169065	PHASE4	COMPLETED	Effectiveness of Clozapine Versus Olanzapine for Treatment-resistant Schizophrenia
NCT00169091	PHASE4	TERMINATED	Clozapine Versus Haloperidol for Treating the First Episode of Schizophrenia
NCT00176423	PHASE4	COMPLETED	Efficacy Study of Galantamine for Cognitive Impairments in Schizophrenia
NCT00176436	PHASE4	COMPLETED	Atomoxetine for Treatment of Weight Gain in Olanzapine or Clozapine Patients
NCT00177008	PHASE4	COMPLETED	Aripiprazole for the Treatment of Schizophrenia With Co-Morbid Social Anxiety