FGFR4

Summary

FGFR4 (fibroblast growth factor receptor 4, HGNC:3691) is a protein-coding gene on chromosome 5q35.2, encoding Fibroblast growth factor receptor 4 (P22455). Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation of lipid metabolism, bile acid biosynthesis, glucose uptake, vitamin D metabolism….

The protein encoded by this gene is a tyrosine kinase and cell surface receptor for fibroblast growth factors. The encoded protein is involved in the regulation of several pathways, including cell proliferation, cell differentiation, cell migration, lipid metabolism, bile acid biosynthesis, vitamin D metabolism, glucose uptake, and phosphate homeostasis. This protein consists of an extracellular region, composed of three immunoglobulin-like domains, a single hydrophobic membrane-spanning segment, and a cytoplasmic tyrosine kinase domain. The extracellular portion interacts with fibroblast growth factors, setting in motion a cascade of downstream signals, ultimately influencing mitogenesis and differentiation.

Source: NCBI Gene 2264 — RefSeq curated summary.

At a glance

• GWAS associations: 108
• Clinical variants (ClinVar): 165 total — 2 pathogenic, 1 likely-pathogenic
• Druggable target: yes — 47 molecules with ChEMBL bioactivity
• Cancer driver (intOGen): loss-of-function (tumor-suppressor-like) across 2 cancer types
• MANE Select transcript: NM_213647

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3691
Approved symbol	FGFR4
Name	fibroblast growth factor receptor 4
Location	5q35.2
Locus type	gene with protein product
Status	Approved
Aliases	JTK2, CD334, TKF
Ensembl gene	ENSG00000160867
Ensembl biotype	protein_coding
OMIM	134935
Entrez	2264

Gene structure

Transcript identifiers

Ensembl transcripts: 59 — 52 protein_coding, 5 retained_intron, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000292408, ENST00000393637, ENST00000393648, ENST00000426612, ENST00000430285, ENST00000483872, ENST00000502906, ENST00000503708, ENST00000507708, ENST00000508139, ENST00000509511, ENST00000510911, ENST00000511076, ENST00000513166, ENST00000513423, ENST00000514472, ENST00000885509, ENST00000885510, ENST00000885511, ENST00000885512, ENST00000885513, ENST00000885514, ENST00000885515, ENST00000885516, ENST00000885517, ENST00000885518, ENST00000885519, ENST00000885520, ENST00000885521, ENST00000885522, ENST00000885523, ENST00000885524, ENST00000885525, ENST00000885526, ENST00000885527, ENST00000885528, ENST00000885529, ENST00000885530, ENST00000885531, ENST00000934141, ENST00000934142, ENST00000934143, ENST00000934144, ENST00000934145, ENST00000934146, ENST00000934147, ENST00000934148, ENST00000934149, ENST00000934150, ENST00000934151, ENST00000934152, ENST00000961676, ENST00000961677, ENST00000961678, ENST00000961679, ENST00000961680, ENST00000961681, ENST00000961682, ENST00000961683

RefSeq mRNA: 5 — MANE Select: NM_213647 NM_001291980, NM_001354984, NM_002011, NM_022963, NM_213647

CCDS: CCDS4410, CCDS4411, CCDS78096

Canonical transcript exons

ENST00000292408 — 18 exons

Exon	Start	End
ENSE00001055082	177093138	177093331
ENSE00001055086	177086915	177087077
ENSE00001055090	177093406	177093551
ENSE00001055094	177097527	177098144
ENSE00001158422	177097292	177097397
ENSE00001158432	177096604	177096741
ENSE00001158459	177095533	177095723
ENSE00001158467	177095330	177095440
ENSE00001158479	177093654	177093775
ENSE00001767417	177096287	177096357
ENSE00003500306	177090390	177090653
ENSE00003546921	177089550	177089693
ENSE00003560536	177092321	177092511
ENSE00003562071	177092646	177092784
ENSE00003590704	177091685	177091808
ENSE00003657503	177090745	177090825
ENSE00003787443	177090938	177091104
ENSE00003790785	177096057	177096179

Expression profiles

Bgee: expression breadth ubiquitous, 185 present calls, max score 96.73.

FANTOM5 (CAGE): breadth broad, TPM avg 7.1994 / max 1558.4127, expressed in 819 samples.

FANTOM5 promoters (9 alternative TSS)

Promoter ID	TPM avg	Samples expressed
60447	4.8930	661
60446	1.6947	535
60448	0.5122	127
60451	0.0429	16
60450	0.0340	18
60452	0.0086	5
60449	0.0062	1
60453	0.0042	1
60454	0.0035	1

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	96.73	gold quality
upper lobe of left lung	UBERON:0008952	95.20	gold quality
right lung	UBERON:0002167	94.99	gold quality
upper lobe of lung	UBERON:0008948	94.36	gold quality
adrenal tissue	UBERON:0018303	93.17	gold quality
body of pancreas	UBERON:0001150	93.16	gold quality
mucosa of transverse colon	UBERON:0004991	93.15	gold quality
metanephros cortex	UBERON:0010533	92.92	gold quality
liver	UBERON:0002107	90.47	gold quality
left ovary	UBERON:0002119	90.12	gold quality
small intestine Peyer’s patch	UBERON:0003454	89.00	gold quality
lung	UBERON:0002048	88.88	gold quality
lower lobe of lung	UBERON:0008949	88.57	gold quality
transverse colon	UBERON:0001157	88.45	gold quality
metanephros	UBERON:0000081	88.32	gold quality
right ovary	UBERON:0002118	88.17	gold quality
spleen	UBERON:0002106	87.83	gold quality
right adrenal gland	UBERON:0001233	87.62	gold quality
small intestine	UBERON:0002108	87.59	gold quality
adult mammalian kidney	UBERON:0000082	87.48	gold quality
right adrenal gland cortex	UBERON:0035827	87.32	gold quality
metanephric glomerulus	UBERON:0004736	86.19	gold quality
renal glomerulus	UBERON:0000074	85.97	gold quality
gall bladder	UBERON:0002110	85.92	gold quality
pancreas	UBERON:0001264	85.83	gold quality
cortex of kidney	UBERON:0001225	85.41	gold quality
left adrenal gland cortex	UBERON:0035825	85.14	gold quality
left adrenal gland	UBERON:0001234	84.95	gold quality
ovary	UBERON:0000992	84.38	gold quality
adrenal cortex	UBERON:0001235	84.05	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.60

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

1 targets.

Target	Regulation
FGFR4	Activation

Upstream regulators (CollecTRI, top): FGFR4, HNF1A, IKZF1, MYC, PAX3, POU1F1, SP1, SP3

miRNA regulators (miRDB)

25 targeting FGFR4, 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-3613-3P	100.00	76.36	7965
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-497-5P	99.92	71.83	2674
HSA-MIR-15A-5P	99.90	72.80	2787
HSA-MIR-15B-5P	99.90	72.78	2798
HSA-MIR-16-5P	99.90	72.80	2780
HSA-MIR-195-5P	99.90	72.81	2805
HSA-MIR-6838-5P	99.89	71.94	2690
HSA-MIR-424-5P	99.89	71.90	2641
HSA-MIR-6779-5P	99.70	65.76	2363
HSA-MIR-6722-3P	99.45	67.62	1919
HSA-MIR-32-3P	99.36	68.20	2517
HSA-MIR-133A-5P	99.28	69.13	941
HSA-MIR-491-5P	99.13	65.98	1468
HSA-MIR-3922-5P	98.77	66.53	1059
HSA-MIR-330-5P	98.73	67.63	1788
HSA-MIR-6849-3P	97.25	64.57	1371
HSA-MIR-4732-3P	97.15	65.45	881
HSA-MIR-6772-3P	97.04	65.89	784
HSA-MIR-6736-3P	96.98	65.22	1342
HSA-MIR-6508-3P	96.73	65.48	576
HSA-MIR-4652-5P	96.46	64.22	553
HSA-MIR-122-3P	94.51	65.61	75

Literature-anchored findings (GeneRIF, showing 40)

• distribution in normal endocrine cells and related tumors of the gastroenteropancreatic system; immunoreactive in rectal L cells and in pancreatic B, PP, and A cells (PMID:11759058)
• Cancer progression and tumor cell motility are associated with the FGFR4 Arg(388) allele. (PMID:11830541)
• FGFR4 expression in astrocytomas correlates with median survival times of the patients. (PMID:11958417)
• findings suggest a novel transcriptional contribution of Ikaros with Ets and Sp1 in regulation of FGFR4 in the pituitary (PMID:11981041)
• Differences in spatial patterns of FGFR expression in normal skin may generate functional diversity in response to FGFs, and in wounded skin FGFs may function in wound healing via induced FGFRs. (PMID:12373339)
• recognition of cryptic promoter in intron 4 by pituitary tumor AP-2alpha (PMID:12642581)
• Fibroblast growth factor receptor 4 (FGFR4) is associated with a poor prognosis in breast cancer patients. (PMID:12815007)
• G388R mutation of the FGFR4 gene is not relevant for breast cancer prognosis (PMID:14710228)
• Role for pituitary tumor-derived FGFR4 in pituitary tumorigenesis in a majority of human pituitary adenomas. Detection of FGFR4 cytoplasmic staining may provide ancillary diagnostic tool in diagnosis of pituitary adenoma, particularly in equivocal cases. (PMID:15070963)
• a tumor-derived FGFR4 isoform provides a novel mechanism beyond ligand independence that explains the pathobiology of proliferative and infiltrative but nonmetastatic neoplasms. (PMID:15231874)
• the FGFR-4 Arg388 allele is associated with both an increased incidence and clinical aggressiveness of prostate cancer (PMID:15448004)
• FGFR-4 may have a role in human thyroid cancer cell progression (PMID:15564323)
• Transgenic hepatocyte FGFR4 may contribute to the repression of bile acid synthesis through c-Jun N-terminal kinase (JNK) signaling but is not required for activation of JNK signaling by bile acids. (PMID:15750181)
• FGFR4 polymorphism may not be relevant in predicting nodal involvement of breast cancer or colon cancer patients. (PMID:16012724)
• Data indicate that after endocytosis, fibroblast growth factor receptor (FGFR)4 and its bound ligand, FGF1, are sorted mainly to the recycling compartment, whereas FGFR1-3 with ligand are sorted mainly to degradation in the lysosomes. (PMID:16091423)
• We conclude that FGFR4 germline polymorphism G388 suppresses cell motility of invasive breast cancer cells by altering signalling pathways and the expression of genes that are required for metastasis. (PMID:16109476)
• For the first time in humans, the expression of basic fibroblast growth factor (bFGF) and its receptors FGFR-2, FGFR-3, and FGFR-4 has been documented in ovaries of second- and third-trimester fetuses. (PMID:16210019)
• results suggest the majority of gain-of-function mutations within kinase genes in the EGFR signaling pathway have already been identified. Our findings also implicate FGFR4 in the pathogenesis of a subset of lung adenocarcinomas (PMID:17487277)
• little evidence to support the tenet that the FGFR4 Gly388Arg polymorphism is a clinically useful marker for lung cancer prognosis (PMID:17519899)
• Fibroblast growth factor FGF19 and its cognate receptor FGFR4 are coexpressed in primary human liver, lung, and colon tumors and xenograft tissues and in a subset of human colon cancer cell lines, where their interactions are important for tumor growth. (PMID:17599042)
• FGFR4 plays essential roles in systemic lipid and glucose homeostasis, as seen in knockout and transgenic mice. (PMID:17664243)
• FGFR4 expression is associated with invasive tumours in patients with GH-secreting pituitary adenomas. (PMID:18070145)
• High FGFR4 mRNA levels were associated with failure on tamoxifen therapy in patients with recurrent breast cancer (PMID:18310279)
• The FGFR4 Gly388Arg polymorphism had consistent associations with survival outcomes in head and neck neoplasms. (PMID:18349267)
• a marker has been identified that predicts the risk to develop Head and Neck Squamous Cell Carcinoma and possibly the sensitivity to cisplatin as well as a novel mutation in the FGFR4 gene. (PMID:18487077)
• FGF19/FGFR4 cross-talk with beta-catenin and that pathway intervention reduces tumor growth. (PMID:18593907)
• The increased receptor stability and sustained FGFR-4 signaling occur in most human prostate cancers due to either the presence of a common genetic polymorphism or the expression of a protein that stabilizes FGFR-4. (PMID:18670643)
• FGFR4 Arg allele of the Gly388Arg polymorphism and the G allele of the rs2011077 polymorphism have a significant impact on the development of prostate cancer and benign prostatic hyperplasia (PMID:18756523)
• the role of FGFR4 in disease risk and outcomes at a population-based level appears to be minor. (PMID:18762813)
• FGFR4 polymorphism is a prognostic marker for advanced NSCLC in Japanese patients. (PMID:18949411)
• FGFR4 contributes significantly to hepatocellular carcinoma progression by modulating alpha-fetoprotein secretion, proliferation and anti-apoptosis. (PMID:19008009)
• FGF15/FGFR4 integrates growth factor signaling with hepatic bile acid metabolism and insulin action (PMID:19237543)
• Resistance to chemotherapy is associated with fibroblast growth factor receptor 4 up-regulation. (PMID:19240166)
• FGFR4 Gly388Arg polymorphism is associated with lung cancer. (PMID:19296538)
• Fluorescent in situ hybridisation analysis on FGFR4, ETS2 and brachyury failed to show either amplification or translocation for ERG and ETS2 loci (PMID:19407855)
• Authors did not detect any contribution of genetic variants in the FGFR2 or FGFR4 genes to inherited predisposition to skin cancer among Caucasian women. (PMID:19500394)
• Higher FGFR4 expression in RMS tumors was associated with advanced-stage cancer and poor survival, while FGFR4 knockdown in a human RMS cell line reduced tumor growth and experimental lung metastases when the cells were transplanted into mice (PMID:19809159)
• The single nucleotide polymorphism Gly(388)Arg in FGFR4 is not associated with increased risk of prostate cancer in Scottish men. (PMID:19918264)
• Studies show that FGFR4 presents an option for further mutational screening in tumours and is an attractive cancer target with the therapeutic potential. (PMID:19946327)
• activation of FGFR4 is the mechanism whereby FGF19 can increase hepatocyte proliferation and induce hepatocellular carcinoma formation. (PMID:20018895)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Fgfr4	ENSMUSG00000005320
rattus_norvegicus	Fgfr4	ENSRNOG00000016763

Paralogs (53): INSRR (ENSG00000027644), MUSK (ENSG00000030304), FLT4 (ENSG00000037280), EPHA3 (ENSG00000044524), ROS1 (ENSG00000047936), LTK (ENSG00000062524), ERBB3 (ENSG00000065361), TIE1 (ENSG00000066056), FGFR2 (ENSG00000066468), FGFR3 (ENSG00000068078), EPHA8 (ENSG00000070886), FGFR1 (ENSG00000077782), EPHA6 (ENSG00000080224), TYRO3 (ENSG00000092445), FLT1 (ENSG00000102755), MET (ENSG00000105976), EPHB6 (ENSG00000106123), PDGFRB (ENSG00000113721), EPHA4 (ENSG00000116106), TEK (ENSG00000120156), FLT3 (ENSG00000122025), KDR (ENSG00000128052), EPHB2 (ENSG00000133216), PDGFRA (ENSG00000134853), EPHA7 (ENSG00000135333), IGF1R (ENSG00000140443), NTRK3 (ENSG00000140538), ERBB2 (ENSG00000141736), EPHA2 (ENSG00000142627), EPHA5 (ENSG00000145242), EGFR (ENSG00000146648), EPHA1 (ENSG00000146904), NTRK2 (ENSG00000148053), MERTK (ENSG00000153208), EPHB1 (ENSG00000154928), KIT (ENSG00000157404), DDR2 (ENSG00000162733), RYK (ENSG00000163785), MST1R (ENSG00000164078), LMTK2 (ENSG00000164715)

Protein

Protein identifiers

Fibroblast growth factor receptor 4 — P22455 (reviewed: P22455)

All UniProt accessions (8): P22455, B5A964, D6R9V0, D6RG06, D6RJD4, E7EWF4, H0Y9P2, J3KPQ0

UniProt curated annotations — full annotation on UniProt →

Function. Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation of lipid metabolism, bile acid biosynthesis, glucose uptake, vitamin D metabolism and phosphate homeostasis. Required for normal down-regulation of the expression of CYP7A1, the rate-limiting enzyme in bile acid synthesis, in response to FGF19. Phosphorylates PLCG1 and FRS2. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Promotes SRC-dependent phosphorylation of the matrix protease MMP14 and its lysosomal degradation. FGFR4 signaling is down-regulated by receptor internalization and degradation; MMP14 promotes internalization and degradation of FGFR4. Mutations that lead to constitutive kinase activation or impair normal FGFR4 inactivation lead to aberrant signaling.

Subunit / interactions. Monomer. Homodimer after ligand binding. Interacts with FGF1, FGF2, FGF4, FGF6, FGF8, FGF9, FGF16, FGF17, FGF18, FGF19, FGF21 and FGF23 (in vitro). Binding affinity for FGF family members is enhanced by interactions between FGFs and heparan sulfate proteoglycans. Interacts with KLB; this strongly increases the affinity for FGF19 and FGF23. Affinity for FGF19 is strongly increased by KLB and sulfated glycosaminoglycans. KLB and KL both interact with the core-glycosylated FGFR4 in the endoplasmic reticulum and promote its degradation, so that only FGFR4 with fully mature N-glycans is expressed at the cell surface. Identified in a complex with NCAM1, CDH2, PLCG1, FRS2, SRC, SHC1, GAP43 and CTTN. Interacts with MMP14 and HIP1. Interacts with STAT3.

Subcellular location. Cell membrane. Endosome. Endoplasmic reticulum Secreted.

Tissue specificity. Expressed in gastrointestinal epithelial cells, pancreas, and gastric and pancreatic cancer cell lines.

Post-translational modifications. N-glycosylated. Full maturation of the glycan chains in the Golgi is essential for high affinity interaction with FGF19. Ubiquitinated. Subject to proteasomal degradation when not fully glycosylated. Autophosphorylated. Binding of FGF family members together with heparan sulfate proteoglycan or heparin promotes receptor dimerization and autophosphorylation on tyrosine residues. Autophosphorylation occurs in trans between the two FGFR molecules present in the dimer.

Disease relevance. FGFR4 variants may be involved in the pathogenesis of various cancers. Variant Arg-388 predisposes cancer patients to accelerated disease progression and may be associated with poor prognosis. It has been found in prostate cancer as well as cancers of the breast, colon, head and neck, larynx, lung, skin.

Activity regulation. Present in an inactive conformation in the absence of bound ligand. Ligand binding leads to dimerization and activation by autophosphorylation on tyrosine residues.

Similarity. Belongs to the protein kinase superfamily. Tyr protein kinase family. Fibroblast growth factor receptor subfamily.

Isoforms (2)

UniProt ID	Names	Canonical?
P22455-1	1	yes
P22455-2	2, Soluble-form

RefSeq proteins (5): NP_001278909, NP_001341913, NP_002002, NP_075252, NP_998812* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR001245	Ser-Thr/Tyr_kinase_cat_dom	Domain
IPR003598	Ig_sub2	Domain
IPR003599	Ig_sub	Domain
IPR007110	Ig-like_dom	Domain
IPR008266	Tyr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR013098	Ig_I-set	Domain
IPR013783	Ig-like_fold	Homologous_superfamily
IPR016248	FGF_rcpt_fam	Family
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR020635	Tyr_kinase_cat_dom	Domain
IPR036179	Ig-like_dom_sf	Homologous_superfamily
IPR050122	RTK	Family

Pfam: PF07679, PF07714, PF13927

Enzyme classification (BRENDA):

• EC 2.7.10.1 — receptor protein-tyrosine kinase (BRENDA: 44 organisms, 214 substrates, 574 inhibitors, 11 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

4 substrates with measured Km, best-characterized 4. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.0011–0.129	4
AC-DYFE-6-CHLORO-W-NHME	0.0051	1
AC-DYFGW-NHME	0.07	1
YFEW	0.232	1

Catalyzed reactions (Rhea), 1 shown:

• L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)

UniProt features (94 total): strand 30, helix 17, sequence variant 10, modified residue 5, glycosylation site 5, turn 5, domain 4, disulfide bond 3, sequence conflict 3, binding site 2, topological domain 2, mutagenesis site 2, signal peptide 1, chain 1, active site 1, splice variant 1, transmembrane region 1, region of interest 1

Structure

Experimental structures (PDB)

52 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
8KH9	X-RAY DIFFRACTION	1.42
8KH8	X-RAY DIFFRACTION	1.49
4QQT	X-RAY DIFFRACTION	1.5
8KH7	X-RAY DIFFRACTION	1.52
6JPE	X-RAY DIFFRACTION	1.6
8KH6	X-RAY DIFFRACTION	1.62
4QQJ	X-RAY DIFFRACTION	1.68
4XCU	X-RAY DIFFRACTION	1.71
4UXQ	X-RAY DIFFRACTION	1.85
6NVH	X-RAY DIFFRACTION	1.9
6V9C	X-RAY DIFFRACTION	1.9
4QRC	X-RAY DIFFRACTION	1.9
8XLQ	X-RAY DIFFRACTION	1.95
7V29	X-RAY DIFFRACTION	1.98
7YC3	X-RAY DIFFRACTION	1.99
6NVG	X-RAY DIFFRACTION	1.99
6IUP	X-RAY DIFFRACTION	2
7DTZ	X-RAY DIFFRACTION	2.01
9K0J	X-RAY DIFFRACTION	2.07
7WCT	X-RAY DIFFRACTION	2.11
6NVI	X-RAY DIFFRACTION	2.12
6YI8	X-RAY DIFFRACTION	2.13
6J6Y	X-RAY DIFFRACTION	2.15
7WCX	X-RAY DIFFRACTION	2.17
4QQ5	X-RAY DIFFRACTION	2.2
7YBX	X-RAY DIFFRACTION	2.23
9K0I	X-RAY DIFFRACTION	2.24
7YBP	X-RAY DIFFRACTION	2.24
7F3M	X-RAY DIFFRACTION	2.29
6IUO	X-RAY DIFFRACTION	2.3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P22455-F1	74.30	0.38

Antibody-complex structures (SAbDab): 1 — 6J6Y

Functional residue map

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

Catalytic / active sites (1): 612 (proton acceptor)

Ligand- & substrate-binding residues (2): 473–481; 503

Post-translational modifications (5): 390, 573, 642, 643, 754

Disulfide bonds (3): 57–101, 172–224, 271–333

Glycosylation sites (5): 112, 258, 290, 311, 322

Mutagenesis-validated functional residues (2):

Position	Phenotype
503	loss of kinase activity.
754	loss of interaction with plcg1.

Function

Pathways and Gene Ontology

Reactome pathways

14 pathways

ID	Pathway
R-HSA-109704	PI3K Cascade
R-HSA-1257604	PIP3 activates AKT signaling
R-HSA-1307965	betaKlotho-mediated ligand binding
R-HSA-1839128	FGFR4 mutant receptor activation
R-HSA-190322	FGFR4 ligand binding and activation
R-HSA-2219530	Constitutive Signaling by Aberrant PI3K in Cancer
R-HSA-5654228	Phospholipase C-mediated cascade; FGFR4
R-HSA-5654712	FRS-mediated FGFR4 signaling
R-HSA-5654719	SHC-mediated cascade:FGFR4
R-HSA-5654720	PI-3K cascade:FGFR4
R-HSA-5654733	Negative regulation of FGFR4 signaling
R-HSA-5655291	Signaling by FGFR4 in disease
R-HSA-5673001	RAF/MAP kinase cascade
R-HSA-6811558	PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling

MSigDB gene sets: 285 (showing top): REACTOME_SIGNALING_BY_INSULIN_RECEPTOR, GOBP_POSITIVE_REGULATION_OF_DNA_BIOSYNTHETIC_PROCESS, GOBP_STEROL_HOMEOSTASIS, KEGG_MAPK_SIGNALING_PATHWAY, REACTOME_SIGNALING_BY_FGFR, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GOBP_POSITIVE_REGULATION_OF_MAPK_CASCADE, KYNG_DNA_DAMAGE_DN, HNF1_Q6, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GGGTGGRR_PAX4_03, GOBP_KETONE_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_BIOSYNTHETIC_PROCESS, GOBP_REGULATION_OF_EXTRACELLULAR_MATRIX_ORGANIZATION, SHEPARD_BMYB_MORPHOLINO_DN

GO Biological Process (19): positive regulation of cell population proliferation (GO:0008284), fibroblast growth factor receptor signaling pathway (GO:0008543), positive regulation of gene expression (GO:0010628), regulation of extracellular matrix disassembly (GO:0010715), cell migration (GO:0016477), peptidyl-tyrosine phosphorylation (GO:0018108), regulation of lipid metabolic process (GO:0019216), glucose homeostasis (GO:0042593), cholesterol homeostasis (GO:0042632), positive regulation of catalytic activity (GO:0043085), positive regulation of proteolysis (GO:0045862), protein autophosphorylation (GO:0046777), phosphate ion homeostasis (GO:0055062), positive regulation of ERK1 and ERK2 cascade (GO:0070374), regulation of bile acid biosynthetic process (GO:0070857), positive regulation of DNA biosynthetic process (GO:2000573), protein phosphorylation (GO:0006468), regulation of gene expression (GO:0010468), positive regulation of MAPK cascade (GO:0043410)

GO Molecular Function (11): fibroblast growth factor receptor activity (GO:0005007), ATP binding (GO:0005524), heparin binding (GO:0008201), fibroblast growth factor binding (GO:0017134), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein tyrosine kinase activity (GO:0004713), transmembrane receptor protein tyrosine kinase activity (GO:0004714), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (9): extracellular region (GO:0005576), endosome (GO:0005768), endoplasmic reticulum (GO:0005783), Golgi apparatus (GO:0005794), plasma membrane (GO:0005886), transport vesicle (GO:0030133), signaling receptor complex (GO:0043235), cell-cell junction (GO:0005911), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-10 pathways:

Category	Pathways
Downstream signaling of activated FGFR4	4
Signaling by FGFR4	2
IRS-mediated signalling	1
Intracellular signaling by second messengers	1
FGFR4 ligand binding and activation	1
Signaling by FGFR4 in disease	1
PI3K/AKT Signaling in Cancer	1
Signaling by FGFR in disease	1
MAPK1/MAPK3 signaling	1
Negative regulation of the PI3K/AKT network	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
endomembrane system	4
gene expression	2
positive regulation of macromolecule biosynthetic process	2
protein phosphorylation	2
catalytic activity	2
cellular anatomical structure	2
cytoplasmic vesicle	2
cytoplasm	2
intracellular membrane-bounded organelle	2
cell population proliferation	1
regulation of cell population proliferation	1
positive regulation of cellular process	1
cell surface receptor protein tyrosine kinase signaling pathway	1
cellular response to fibroblast growth factor stimulus	1
regulation of gene expression	1
extracellular matrix disassembly	1
regulation of extracellular matrix organization	1
cell motility	1
peptidyl-tyrosine modification	1
lipid metabolic process	1
regulation of primary metabolic process	1
carbohydrate homeostasis	1
sterol homeostasis	1
positive regulation of molecular function	1
regulation of catalytic activity	1
proteolysis	1
regulation of proteolysis	1
positive regulation of protein metabolic process	1
inorganic ion homeostasis	1
positive regulation of MAPK cascade	1
ERK1 and ERK2 cascade	1
regulation of ERK1 and ERK2 cascade	1
bile acid biosynthetic process	1
regulation of ketone metabolic process	1
regulation of steroid biosynthetic process	1
regulation of small molecule metabolic process	1
positive regulation of DNA metabolic process	1
DNA biosynthetic process	1
regulation of DNA biosynthetic process	1
phosphorylation	1

Protein interactions and networks

STRING

2067 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FGFR4	KLB	Q86Z14	999
FGFR4	FGF19	O95750	998
FGFR4	FGF1	P05230	994
FGFR4	FGF6	P10767	993
FGFR4	FGF2	P09038	993
FGFR4	FGF4	P08620	992
FGFR4	FGF8	P55075	991
FGFR4	FGF18	O76093	990
FGFR4	FGF9	P31371	990
FGFR4	FGF17	O60258	989
FGFR4	FGF13	Q92913	989
FGFR4	KL	Q9UEF7	987
FGFR4	FGF5	P12034	986
FGFR4	FGF23	Q9GZV9	985
FGFR4	FGF7	P21781	983
FGFR4	FGF3	P11487	983

IntAct

169 interactions, top by confidence:

A	B	Type	Score
CDK9	AIP	psi-mi:“MI:0914”(association)	0.730
CRIPTO	AIP	psi-mi:“MI:0914”(association)	0.640
FBXO6	MAN2B1	psi-mi:“MI:0914”(association)	0.640
PDGFRB	PIK3R2	psi-mi:“MI:0914”(association)	0.610
FGFR4	SDC2	psi-mi:“MI:0407”(direct interaction)	0.560
TGFBR3	FGFR4	psi-mi:“MI:0407”(direct interaction)	0.560
FGFR4	FGFR1	psi-mi:“MI:0915”(physical association)	0.540
SLC39A5	TMEM223	psi-mi:“MI:0914”(association)	0.530
TMEM30B	KLRG2	psi-mi:“MI:0914”(association)	0.530
FCGRT	GOLIM4	psi-mi:“MI:0914”(association)	0.530
TMX1	NRP1	psi-mi:“MI:0914”(association)	0.530
CLEC4A	SEMA7A	psi-mi:“MI:0914”(association)	0.530
MRAP2	GOLIM4	psi-mi:“MI:0914”(association)	0.530
CCL22	PLXNA2	psi-mi:“MI:0914”(association)	0.530
FBXO2	TMEM131L	psi-mi:“MI:0914”(association)	0.530
C1orf54	EXTL3	psi-mi:“MI:0914”(association)	0.530
PTPN11	FGFR4	psi-mi:“MI:0915”(physical association)	0.520
RET	FGFR4	psi-mi:“MI:0915”(physical association)	0.500
FGFR4	FGF1	psi-mi:“MI:2364”(proximity)	0.480
	BIN1	psi-mi:“MI:0914”(association)	0.460
FGF19	FGFR4	psi-mi:“MI:0407”(direct interaction)	0.440
	FGFR4	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (485): ANGPTL4 (Two-hybrid), BLID (Two-hybrid), CASC3 (Two-hybrid), DIRAS3 (Two-hybrid), EPSTI1 (Two-hybrid), ERRFI1 (Two-hybrid), FAM84B (Two-hybrid), GLCE (Two-hybrid), MTA3 (Two-hybrid), OSGIN1 (Two-hybrid), PDLIM2 (Two-hybrid), PSMC3IP (Two-hybrid), RASL10B (Two-hybrid), RNF20 (Two-hybrid), SCGB3A1 (Two-hybrid)

ESM2 similar proteins: A0A8P0N4K0, A2AB59, B4F7F3, D3YZU1, D3ZD05, O35681, O75427, O95382, P22455, P22607, P40748, P55144, P70218, Q06418, Q14160, Q1LZH7, Q2PS20, Q32P44, Q495M9, Q4ACU6, Q4H4B6, Q505F5, Q5F488, Q61851, Q63ZY3, Q6P9K8, Q6TLK4, Q6ZUM4, Q7KRY7, Q80T11, Q80U72, Q8BH60, Q8BX02, Q8N1G4, Q8TE68, Q8VC03, Q8VHK1, Q8VHK2, Q8WXD9, Q8WXE0

Diamond homologs: A0M8R7, A0M8S8, A1X150, B3MH43, B3NS99, B4GBH0, B4HNW4, B4KPU0, B4MR28, B4P5Q9, B4QC63, O15146, O42127, O73798, O76997, P00529, P04629, P06213, P08069, P08581, P08922, P08941, P14616, P14617, P15209, P16056, P22455, P22607, P23049, P24062, P24786, P35739, P42681, P42682, P97523, Q00PJ8, Q03146, Q03351, Q04912, Q05688

SIGNOR signaling

18 interactions.

A	Effect	B	Mechanism
FGFR4	up-regulates	FGFR4	phosphorylation
FGF1	up-regulates	FGFR4	binding
FGF2	up-regulates	FGFR4	binding
FGF4	up-regulates	FGFR4	binding
FGF6	up-regulates	FGFR4	binding
BGJ-398	down-regulates	FGFR4	“chemical inhibition”
FGFR4	“up-regulates activity”	STAT1	phosphorylation
FGFR4	“up-regulates activity”	STAT3	phosphorylation
PAX7-FOXO1	“up-regulates quantity by expression”	FGFR4	“transcriptional regulation”
PAX3-FOXO1	“up-regulates quantity by expression”	FGFR4	“transcriptional regulation”
PAX3	“up-regulates quantity by expression”	FGFR4	“transcriptional regulation”
ponatinib	“down-regulates activity”	FGFR4	“chemical inhibition”
FGFR4	“down-regulates activity”	STK4	phosphorylation
FGFR4	“up-regulates activity”	FRS2	phosphorylation
FGFR4	“up-regulates activity”	FGFR4	phosphorylation
nintedanib	“down-regulates activity”	FGFR4	“chemical inhibition”
FGFR4	“up-regulates activity”	GLO1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 183 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
HS-GAG degradation	5	19.4×	8e-04
Negative regulation of FGFR1 signaling	5	14.4×	2e-03
HS-GAG biosynthesis	5	13.5×	2e-03
PI3K Cascade	6	12.8×	1e-03
Constitutive Signaling by Aberrant PI3K in Cancer	9	8.9×	2e-04
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	11	8.3×	3e-05
PIP3 activates AKT signaling	13	6.8×	3e-05
RAF/MAP kinase cascade	10	4.8×	3e-03

GO biological processes:

GO term	Partners	Fold	FDR
positive regulation of SMAD protein signal transduction	5	11.6×	9e-03
cytokine-mediated signaling pathway	10	7.9×	2e-04
positive regulation of MAPK cascade	13	6.3×	7e-05
positive regulation of cell migration	15	5.6×	6e-05
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	11	5.2×	3e-03
positive regulation of ERK1 and ERK2 cascade	10	5.2×	5e-03

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: loss-of-function (tumor-suppressor-like) across 2 cancer types — GBM, UCEC.

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	1
Uncertain significance	101
Likely benign	15
Benign	11

Top pathogenic / likely-pathogenic (3)

Variant ID	HGVS	Classification
2685189	GRCh37/hg19 5q35.2(chr5:176483840-176588195)x1	Pathogenic
830214	NC_000005.10:g.(177090796_177094455)_(177346090_177352856)dup	Pathogenic
690278	Single allele	Likely pathogenic

SpliceAI

2933 predictions. Top by Δscore:

Variant	Effect	Δscore
5:177089681:G:GT	donor_gain	1.0000
5:177091101:TCGGG:T	donor_loss	1.0000
5:177091102:CGGGT:C	donor_loss	1.0000
5:177091103:GG:G	donor_gain	1.0000
5:177091104:GG:G	donor_gain	1.0000
5:177091105:G:C	donor_loss	1.0000
5:177091105:G:GG	donor_gain	1.0000
5:177091106:T:G	donor_loss	1.0000
5:177091804:GCTGG:G	donor_gain	1.0000
5:177091807:GG:G	donor_gain	1.0000
5:177091808:GG:G	donor_gain	1.0000
5:177092318:CA:C	acceptor_loss	1.0000
5:177092319:A:AG	acceptor_gain	1.0000
5:177092319:AGAGC:A	acceptor_gain	1.0000
5:177092320:G:GC	acceptor_loss	1.0000
5:177092320:G:GG	acceptor_gain	1.0000
5:177092320:GA:G	acceptor_gain	1.0000
5:177092320:GAGC:G	acceptor_gain	1.0000
5:177092320:GAGCG:G	acceptor_gain	1.0000
5:177092498:TGC:T	donor_gain	1.0000
5:177092511:GGTAA:G	donor_loss	1.0000
5:177092513:T:A	donor_loss	1.0000
5:177092644:A:AG	acceptor_gain	1.0000
5:177092644:A:AT	acceptor_loss	1.0000
5:177092645:G:GA	acceptor_gain	1.0000
5:177092781:CCAGG:C	donor_loss	1.0000
5:177092783:AGG:A	donor_loss	1.0000
5:177092784:GGTGA:G	donor_loss	1.0000
5:177092786:T:A	donor_loss	1.0000
5:177093113:T:TA	acceptor_gain	1.0000

AlphaMissense

5139 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
5:177091010:T:C	F170S	1.000
5:177091051:T:A	W184R	1.000
5:177091051:T:C	W184R	1.000
5:177091052:G:C	W184S	1.000
5:177091053:G:C	W184C	1.000
5:177091053:G:T	W184C	1.000
5:177091745:T:G	Y222D	1.000
5:177091751:T:C	C224R	1.000
5:177091753:C:G	C224W	1.000
5:177091797:T:C	L239P	1.000
5:177092339:C:A	P249H	1.000
5:177092339:C:G	P249R	1.000
5:177092404:T:C	C271R	1.000
5:177092406:C:G	C271W	1.000
5:177092440:T:A	W283R	1.000
5:177092440:T:C	W283R	1.000
5:177092442:G:C	W283C	1.000
5:177092442:G:T	W283C	1.000
5:177092444:T:C	L284P	1.000
5:177092724:T:C	C333R	1.000
5:177092726:C:G	C333W	1.000
5:177092738:T:A	N337K	1.000
5:177092738:T:G	N337K	1.000
5:177096070:A:C	D612A	1.000
5:177096070:A:T	D612V	1.000
5:177096086:T:A	N617K	1.000
5:177096086:T:G	N617K	1.000
5:177096124:A:T	D630V	1.000
5:177096305:T:A	W655R	1.000
5:177096305:T:C	W655R	1.000

dbSNP variants (sampled 300 via entrez): RS1000336443 (5:177091329 A>G), RS1000446621 (5:177094995 C>A,T), RS1001350514 (5:177086904 C>A,G,T), RS1001478338 (5:177095783 G>A), RS1001742866 (5:177089965 T>C), RS1001780664 (5:177087083 C>G), RS1001783121 (5:177097797 G>A), RS1002197930 (5:177094106 C>A,T), RS1002266150 (5:177094133 C>T), RS1002337401 (5:177088392 G>C), RS1002912652 (5:177091591 A>G), RS1003074764 (5:177088812 C>G), RS1003663443 (5:177087271 C>A,T), RS1003746076 (5:177087056 C>T), RS1003854276 (5:177096474 G>A,C)

Disease associations

OMIM: gene MIM:134935 | disease phenotypes: MIM:236000

GenCC curated gene-disease

Mondo (2): classic Hodgkin lymphoma (MONDO:0009348), 5q35 microduplication syndrome (MONDO:0016461)

Orphanet (2): Classic Hodgkin lymphoma (Orphanet:391), 5q35 microduplication syndrome (Orphanet:228415)

HPO phenotypes

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

GWAS associations

108 associations (top):

Study	Trait	p-value
GCST001574_7	Activated partial thromboplastin time	6.000000e-88
GCST002647_129	Height	2.000000e-20
GCST002782_151	Waist-to-hip ratio adjusted for body mass index	1.000000e-06
GCST002782_152	Waist-to-hip ratio adjusted for body mass index	3.000000e-08
GCST002782_153	Waist-to-hip ratio adjusted for body mass index	5.000000e-07
GCST002782_154	Waist-to-hip ratio adjusted for body mass index	3.000000e-08
GCST003338_7	Waist-to-hip ratio adjusted for body mass index	2.000000e-06
GCST004063_5	Waist circumference adjusted for body mass index	2.000000e-12
GCST004063_83	Waist circumference adjusted for body mass index	6.000000e-10
GCST004500_110	Waist circumference adjusted for BMI (adjusted for smoking behaviour)	4.000000e-14
GCST004500_40	Waist circumference adjusted for BMI (adjusted for smoking behaviour)	9.000000e-11
GCST004500_59	Waist circumference adjusted for BMI (adjusted for smoking behaviour)	2.000000e-06
GCST004501_43	Waist circumference adjusted for BMI (joint analysis main effects and smoking interaction)	8.000000e-14
GCST004501_44	Waist circumference adjusted for BMI (joint analysis main effects and smoking interaction)	3.000000e-09
GCST004501_45	Waist circumference adjusted for BMI (joint analysis main effects and smoking interaction)	2.000000e-06
GCST004503_13	Waist circumference adjusted for BMI in smokers	3.000000e-06
GCST004504_45	Waist circumference adjusted for BMI in non-smokers	5.000000e-10
GCST004504_46	Waist circumference adjusted for BMI in non-smokers	2.000000e-07
GCST004505_54	Waist-to-hip ratio adjusted for BMI (adjusted for smoking behaviour)	4.000000e-07
GCST004505_55	Waist-to-hip ratio adjusted for BMI (adjusted for smoking behaviour)	4.000000e-07
GCST004507_10	Waist-to-hip ratio adjusted for BMI (joint analysis main effects and smoking interaction)	7.000000e-06
GCST004507_39	Waist-to-hip ratio adjusted for BMI (joint analysis main effects and smoking interaction)	5.000000e-06
GCST004562_125	Waist circumference adjusted for body mass index	3.000000e-15
GCST004562_166	Waist circumference adjusted for body mass index	4.000000e-15
GCST004562_205	Waist circumference adjusted for body mass index	1.000000e-07
GCST004562_22	Waist circumference adjusted for body mass index	1.000000e-09
GCST004562_222	Waist circumference adjusted for body mass index	1.000000e-09
GCST004562_99	Waist circumference adjusted for body mass index	8.000000e-10
GCST004563_102	Waist circumference adjusted for BMI (joint analysis main effects and physical activity interaction)	4.000000e-15
GCST004563_168	Waist circumference adjusted for BMI (joint analysis main effects and physical activity interaction)	6.000000e-08

EFO canonical traits (14, from GWAS)

EFO ID	Trait name
EFO:0007788	BMI-adjusted waist-hip ratio
EFO:0007789	BMI-adjusted waist circumference
EFO:0004318	smoking behavior
EFO:0008002	physical activity measurement
EFO:0008007	age at assessment
EFO:0008343	sex interaction measurement
EFO:0004685	hip geometry
EFO:0004341	body fat distribution
EFO:0004511	femoral neck bone geometry
EFO:0003959	cleft lip
EFO:0004509	hemoglobin measurement
EFO:0004614	apolipoprotein A 1 measurement
EFO:0008039	BMI-adjusted hip circumference
EFO:0004980	appendicular lean mass

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL2095217 (PROTEIN FAMILY), CHEMBL3973 (SINGLE PROTEIN), CHEMBL4804255 (PROTEIN COMPLEX), CHEMBL5291679 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

47 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 215,496 (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
CHEMBL1171837	PONATINIB	4	8,955
CHEMBL4297522	PEMIGATINIB	4	2,055
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1289601	LENVATINIB	4	8,784
CHEMBL1834657	INFIGRATINIB PHOSPHATE	4	285
CHEMBL1852688	INFIGRATINIB	4	2,209
CHEMBL2403108	CERITINIB	4	8,551
CHEMBL24828	VANDETANIB	4	42,230
CHEMBL3039504	NINTEDANIB ESYLATE	4	659
CHEMBL3545311	BRIGATINIB	4	5,634
CHEMBL3545376	ERDAFITINIB	4	2,794
CHEMBL3701238	FUTIBATINIB	4	813
CHEMBL477772	PAZOPANIB	4	15,540
CHEMBL535	SUNITINIB	4	79,020
CHEMBL223360	LINIFANIB	3	3,925
CHEMBL276711	SEMAXANIB	3	6,180
CHEMBL377300	BRIVANIB	3	1,721
CHEMBL491473	CEDIRANIB	3	9,098
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL572881	MOTESANIB	3
CHEMBL603469	LESTAURTINIB	3
CHEMBL124660	TANDUTINIB	2
CHEMBL103667	DORAMAPIMOD	2
CHEMBL1721885	SU-014813	2
CHEMBL1738757	REBASTINIB	2
CHEMBL2170582	R-343	2
CHEMBL253969	OSI-632	2
CHEMBL3348846	FEXAGRATINIB	2
CHEMBL3686884	E-7090	2

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

PharmGKB clinical annotations

2 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs351855	Efficacy	3	cyclophosphamide;fluorouracil;methotrexate	Breast Neoplasms
rs351855	Efficacy	3	everolimus	Discontinuation

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs351855	FGFR4	3	1.75	2	everolimus;cyclophosphamide;fluorouracil;methotrexate

GtoPdb / IUPHAR curated pharmacology

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

Target class: catalytic receptor — Type V RTKs: FGF (fibroblast growth factor) receptor family

Most potent curated ligand interactions (20 total), top 20:

Ligand	Action	Affinity	Parameter
TYRA-200	Inhibition	10.0	pKd
FGF-19	Binding	9.0	pKd
roblitinib	Inhibition	8.72	pIC50
BLU-9931	Irreversible inhibition	8.52	pIC50
futibatinib	Inhibition	8.47	pIC50
compound A34 [PMID: 35635004]	Inhibition	8.27	pIC50
erdafitinib	Inhibition	8.25	pIC50
LY2874455	Inhibition	8.22	pIC50
irpagratinib	Inhibition	8.07	pIC50
fisogatinib	Irreversible inhibition	8.06	pIC50
PRN1371	Inhibition	7.71	pIC50
segigratinib	Inhibition	7.29	pIC50
infigratinib	Inhibition	7.22	pIC50
compound 29 [PMID: 36356320]	Inhibition	6.84	pIC50
fexagratinib	Inhibition	6.78	pIC50
zoligratinib	Inhibition	6.54	pIC50
compound 7 [Nguyen et al., 2023]	Inhibition	6.45	pIC50
dabogratinib	Inhibition	6.39	pIC50
nintedanib	Inhibition	6.21	pIC50
tasurgratinib	Inhibition	6.19	pIC50

Binding affinities (BindingDB)

629 measured of 982 human assays (982 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[(3-oxothiomorpholin-4-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.1 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.2 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-[(2R)-1-methoxypropan-2-yl]oxy-2-pyridinyl]-7-formyl-6-[[(4S)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.2 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-(2-oxo-1,3-oxazolidin-3-yl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.2 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(oxetan-2-ylmethoxy)-2-pyridinyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.3 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[[(3S)-3-methyl-5-oxomorpholin-4-yl]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.3 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-6-[[(2-hydroxyacetyl)-methylamino]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.3 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[[(2-methoxyacetyl)-methylamino]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.3 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-(3,5-dimethoxyphenyl)-N-(1H-imidazol-5-ylmethyl)-7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-amine	IC50	0.355 nM	US-9757364: Naphthyridine derivative compounds
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[(3-oxomorpholin-4-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.4 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-6-[[[2-(dimethylamino)acetyl]-methylamino]methyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.4 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
6-[[acetyl(methyl)amino]methyl]-N-[5-cyano-4-[2-(trifluoromethoxy)ethylamino]-2-pyridinyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.4 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-(2-fluoro-3,5-dimethoxyphenyl)-7-(1-methylpyrazol-4-yl)-N-(1H-pyrazol-5-ylmethyl)-1,5-naphthyridin-2-amine	IC50	0.417 nM	US-9757364: Naphthyridine derivative compounds
8-chloro-N-(3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-amine	IC50	0.447 nM	US-9757364: Naphthyridine derivative compounds
N-(3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-amine	IC50	0.501 nM	US-9757364: Naphthyridine derivative compounds
4-(2-fluoro-3,5-dimethoxy-N-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]anilino)butanenitrile	IC50	0.55 nM	US-9757364: Naphthyridine derivative compounds
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[[(3R)-3-methyl-5-oxomorpholin-4-yl]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.6 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-[(2R)-1-methoxypropan-2-yl]oxy-2-pyridinyl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.6 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
(2S)-N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-2-methyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.6 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-(3,5-dimethoxyphenyl)-7-(1-methylpyrazol-4-yl)-N-piperidin-4-yl-1,5-naphthyridin-2-amine	IC50	0.676 nM	US-9757364: Naphthyridine derivative compounds
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.7 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(oxolan-3-yloxy)-2-pyridinyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.7 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.7 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(propan-2-ylamino)-2-pyridinyl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.7 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
(2S)-N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-2-methyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.7 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
2-(N-[8-chloro-7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]-3,5-dimethoxyanilino)ethanol	IC50	0.724 nM	US-9757364: Naphthyridine derivative compounds
3-(N-[8-chloro-7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]-3,5-dimethoxyanilino)propan-1-ol	IC50	0.794 nM	US-9757364: Naphthyridine derivative compounds
N-[4-(4-chloro-2-hydroxybutoxy)-5-cyano-2-pyridinyl]-7-formyl-6-(hydroxymethyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.8 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-[[(1S,2R,3S,4R)-3-(hydroxymethyl)-2-bicyclo[2.2.1]heptanyl]amino]-2-pyridinyl]-7-formyl-6-(hydroxymethyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.8 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[[(3R)-3-hydroxy-2-oxopyrrolidin-1-yl]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.8 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-(2-fluoro-3,5-dimethoxyphenyl)-7-(1-methylpyrazol-4-yl)-N-(1,3-oxazol-2-ylmethyl)-1,5-naphthyridin-2-amine	IC50	0.851 nM	US-9757364: Naphthyridine derivative compounds
N-(3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-7-pyridin-4-yl-1,5-naphthyridin-2-amine	IC50	0.851 nM	US-9757364: Naphthyridine derivative compounds
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[[(3S)-3-hydroxy-2-oxopyrrolidin-1-yl]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	0.9 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N’-(2,6-difluoro-3,5-dimethoxyphenyl)-N-methyl-N’-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]ethane-1,2-diamine	IC50	0.912 nM	US-9757364: Naphthyridine derivative compounds
5-[(2,6-difluoro-3,5-dimethoxy-N-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]anilino)methyl]pyrrolidin-2-one	IC50	0.955 nM	US-9757364: Naphthyridine derivative compounds
N’-(2,6-difluoro-3,5-dimethoxyphenyl)-N’-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]-N-propan-2-ylethane-1,2-diamine	IC50	0.977 nM	US-9757364: Naphthyridine derivative compounds
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-6-(oxolan-3-yl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	1 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
2-[(3,5-dimethoxy-N-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]anilino)methyl]-N,N-dimethylimidazole-1-sulfonamide	IC50	1 nM	US-9757364: Naphthyridine derivative compounds
BGJ398	IC50	1 nM	US-9434697: Pyrimidine FGFR4 inhibitors
5-[(2-fluoro-3,5-dimethoxy-N-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]anilino)methyl]pyrrolidin-2-one	IC50	1.07 nM	US-9757364: Naphthyridine derivative compounds
N-[5-cyano-4-(oxolan-2-ylmethoxy)-2-pyridinyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	1.1 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-6-formyl-2,3-dihydropyrrolo[2,3-b]pyridine-1-carboxamide	IC50	1.1 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-imidazol-1-yl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	1.1 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N’-(2-fluoro-3,5-dimethoxyphenyl)-N’-[7-(1-methylpyrazol-4-yl)-1,5-naphthyridin-2-yl]-N-propan-2-ylethane-1,2-diamine	IC50	1.1 nM	US-9757364: Naphthyridine derivative compounds
N-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1-methylpyrazol-4-yl)-N-(oxolan-2-ylmethyl)-1,5-naphthyridin-2-amine	IC50	1.15 nM	US-9757364: Naphthyridine derivative compounds
1-[3-[4-amino-5-[2-(3,5-dimethoxyphenyl)ethynyl]-4a,7a-dihydropyrrolo[2,3-d]pyrimidin-7-yl]azetidin-1-yl]prop-2-en-1-one	IC50	1.2 nM	US-9108973: 3,5-disubstituted alkynylbenzene compound and salt thereof
N-[5-cyano-4-(4-hydroxy-4-methylpiperidin-1-yl)-2-pyridinyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	1.2 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(oxan-2-ylmethoxy)-2-pyridinyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	1.2 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[(1,1,3-trioxo-1,4-thiazinan-4-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	1.2 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors
N-[5-cyano-4-(2-hydroxyethylamino)-2-pyridinyl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	IC50	1.2 nM	US-9266883: Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors

ChEMBL bioactivities

3418 potent at pChembl≥5 of 3439 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.00	IC50	0.1	nM	CHEMBL3948579
9.70	IC50	0.2	nM	CHEMBL3912731
9.70	IC50	0.2	nM	CHEMBL3968338
9.70	IC50	0.2	nM	CHEMBL3912896
9.70	IC50	0.2	nM	CHEMBL4786195
9.60	IC50	0.25	nM	CHEMBL5194425
9.52	IC50	0.3	nM	CHEMBL3915180
9.52	IC50	0.3	nM	CHEMBL3938786
9.52	IC50	0.3	nM	CHEMBL3924363
9.52	IC50	0.3	nM	CHEMBL3946444
9.49	IC50	0.32	nM	CHEMBL5523644
9.40	IC50	0.4	nM	CHEMBL190161
9.40	IC50	0.4	nM	CHEMBL3968334
9.40	IC50	0.4	nM	CHEMBL3975745
9.40	IC50	0.4	nM	CHEMBL3922033
9.40	IC50	0.4	nM	CHEMBL4744686
9.40	IC50	0.4	nM	CHEMBL4796410
9.40	IC50	0.4	nM	CHEMBL5557389
9.40	IC50	0.4	nM	CHEMBL5991133
9.40	IC50	0.4	nM	PEMIGATINIB
9.38	IC50	0.42	nM	CHEMBL5900451
9.34	IC50	0.46	nM	CHEMBL5505760
9.33	IC50	0.47	nM	ASP-5878
9.30	IC50	0.5	nM	CHEMBL191023
9.30	IC50	0.5	nM	CHEMBL191070
9.30	IC50	0.5	nM	CHEMBL3701239
9.30	IC50	0.5	nM	CHEMBL5194425
9.26	IC50	0.55	nM	CHEMBL4866267
9.24	IC50	0.57	nM	CHEMBL5532250
9.22	IC50	0.6	nM	CHEMBL4110949
9.22	IC50	0.6	nM	CHEMBL4111721
9.22	IC50	0.6	nM	CHEMBL3955196
9.22	IC50	0.6	nM	CHEMBL4754106
9.22	IC50	0.6	nM	CHEMBL5935123
9.21	IC50	0.62	nM	CHEMBL5523440
9.20	IC50	0.63	nM	CHEMBL5556836
9.17	IC50	0.68	nM	CHEMBL5505810
9.15	IC50	0.7	nM	CHEMBL3973588
9.15	IC50	0.7	nM	CHEMBL3959971
9.15	IC50	0.7	nM	CHEMBL3924265
9.15	IC50	0.7	nM	CHEMBL3948578
9.15	IC50	0.7	nM	CHEMBL3940110
9.15	IC50	0.7	nM	CHEMBL4764394
9.15	IC50	0.7	nM	CHEMBL5202677
9.15	IC50	0.7	nM	CHEMBL5186034
9.14	IC50	0.73	nM	CHEMBL5532164
9.14	IC50	0.72	nM	CHEMBL5938900
9.13	IC50	0.74	nM	CHEMBL5875472
9.13	IC50	0.74	nM	CHEMBL5890934
9.12	IC50	0.75	nM	CHEMBL5505915

PubChem BioAssay actives

1129 with measured affinity, of 2628 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
N-[5-cyano-4-(2-methoxyethoxy)-2-pyridinyl]-6-[[(4R)-4-(dimethylamino)-2-oxopyrrolidin-1-yl]methyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0002	uM
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[[(2-methoxyacetyl)-methylamino]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0003	uM
N-[2-[[5-[(1R)-1-(3,5-dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]amino]-3-fluoro-5-(4-morpholin-4-ylpiperidin-1-yl)phenyl]prop-2-enamide	1934922: Inhibition of FGFR4 V550L mutant (unknown origin)	ic50	0.0003	uM
N-[4-(pyrazolo[5,4-b]pyridine-1-carbonyl)phenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0003	uM
6-[[acetyl(methyl)amino]methyl]-N-[5-cyano-4-(propan-2-ylamino)-2-pyridinyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0004	uM
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-6-[(3-oxomorpholin-4-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0004	uM
N-[2-[[6-[2-(2,6-dichloro-3,5-dimethoxyanilino)-3-pyridinyl]pyrimidin-4-yl]amino]-3-methylphenyl]prop-2-enamide	1698525: Inhibition of N-terminal 6x-His tagged FGFR4 catalytic domain (445-753 residues) (unknown origin) using IYGEFKKK substrate and [gamma-32P]-ATP incubated for 30 mins by scintillation counting based paper disk assay	ic50	0.0004	uM
N-[4-[[6-(3,5-dimethoxyphenyl)purin-9-yl]methyl]phenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0004	uM
1-tert-butyl-3-[3-(3,5-dimethoxyphenyl)-7-[4-(4-methylpiperazin-1-yl)butylamino]-1,6-naphthyridin-2-yl]urea	248789: Inhibition of FGF-dependent human umbilical vein endothelial cell proliferation	ic50	0.0004	uM
N-(6-chloro-3-nitro-2-pyridinyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-amine	2105171: Inhibition of N-terminal GST tagged cytoplasmic domain human FGFR4 (460 to 802 residues) expressed in Escherichia coli BL21 (DE3) using CSox as substrate incubated for 240 mins in presence of ATP by hotspot assay	ic50	0.0005	uM
N-[5-[(4-chloropyrrolo[2,3-b]pyridin-1-yl)methyl]-2-fluorophenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0005	uM
N-(6-chloro-3-nitro-2-pyridinyl)-6-(3,5-dimethoxyphenyl)quinazolin-2-amine	2105171: Inhibition of N-terminal GST tagged cytoplasmic domain human FGFR4 (460 to 802 residues) expressed in Escherichia coli BL21 (DE3) using CSox as substrate incubated for 240 mins in presence of ATP by hotspot assay	ic50	0.0005	uM
1-tert-butyl-3-[7-[4-(diethylamino)butylamino]-3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-yl]urea	248925: Inhibition of FGF-stimulated human umbilical vein endothelial cell proliferation	ic50	0.0005	uM
1-tert-butyl-3-[3-(3,5-dimethoxyphenyl)-7-(5-morpholin-4-ylpentylamino)-1,6-naphthyridin-2-yl]urea	248789: Inhibition of FGF-dependent human umbilical vein endothelial cell proliferation	ic50	0.0005	uM
2-[4-[[5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl]amino]pyrazol-1-yl]ethanol	1911609: Inhibition of recombinant FGFR4 (unknown origin) by mobility assay	ic50	0.0005	uM
N-[5-cyano-4-(2-methoxyethoxy)-2-pyridinyl]-6-[[(4S)-4-(dimethylamino)-2-oxopyrrolidin-1-yl]methyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0006	uM
N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-3-methyl-5-[2-(4-methylpiperazin-1-yl)ethyl]phenyl]prop-2-enamide	1773781: Inhibition of N-terminal GST fusion tagged human FGFR4 cytoplasmic domain (460 to 802 end residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate addition and further incubated for 30 mins in presence of ATP at Km concentration by caliper mobility shift assay	ic50	0.0006	uM
N-[4-[(6-chloropurin-9-yl)methyl]phenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0006	uM
2-chloro-N-[4-[(6-chloropurin-9-yl)methyl]phenyl]propanamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0006	uM
N-[4-[[6-(3,4-difluorophenyl)purin-9-yl]methyl]phenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0006	uM
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-6-[(2-oxopyrrolidin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0007	uM
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1409769: Inhibition of FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay	ic50	0.0007	uM
N-[(3S,4S)-3-[[3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-ethyl-2-oxo-1,6-naphthyridin-7-yl]amino]oxan-4-yl]prop-2-enamide	1911528: Inhibition of FGFR4 (unknown origin) using Poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ELISA	ic50	0.0007	uM
N-[2-[[3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-ethyl-2-oxo-1,6-naphthyridin-7-yl]amino]-3-methoxyphenyl]prop-2-enamide	1911528: Inhibition of FGFR4 (unknown origin) using Poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ELISA	ic50	0.0007	uM
N-[5-[(6-bromoindol-1-yl)methyl]-2-fluorophenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0007	uM
N-[5-[(6-chloropurin-9-yl)methyl]-2-fluorophenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0007	uM
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-6-[[methyl(methylsulfonyl)amino]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0008	uM
N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-2-(prop-2-enoylamino)benzamide	1416442: Inhibition of wild type non-phosphorylated N-terminal His6-tagged FGFR4 (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay	ic50	0.0008	uM
N-[5-[(5-chloroimidazo[4,5-b]pyridin-3-yl)methyl]-2-fluorophenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0008	uM
N-(2,2-difluoroethyl)-1-[[4-fluoro-3-(prop-2-enoylamino)phenyl]methyl]benzotriazole-4-carboxamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0008	uM
N-[4-[(6-chloropurin-9-yl)methyl]phenyl]-2-methylprop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0008	uM
Infigratinib	1416443: Inhibition of non-phosphorylated N-terminal His6-tagged FGFR4 C552A mutant (G442 to E753 residues) (unknown origin) expressed in sf9 cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay	ic50	0.0008	uM
N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-6-(difluoromethyl)-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0009	uM
6-[[acetyl(ethyl)amino]methyl]-N-[5-cyano-4-(2-methoxyethylamino)-2-pyridinyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0009	uM
N-[5-cyano-4-(2-methoxyethoxy)-2-pyridinyl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0009	uM
N-[5-cyano-4-(2-methoxyethoxy)-2-pyridinyl]-6-[[(3S)-3-(dimethylamino)-2-oxopyrrolidin-1-yl]methyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0009	uM
N-[5-cyano-4-(2-methoxyethoxy)-2-pyridinyl]-6-[[[2-(dimethylamino)acetyl]-methylamino]methyl]-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0009	uM
2,4-difluoro-N-methoxy-5-[[5-propan-2-yl-6-(5-propan-2-yl-1,3,4-oxadiazol-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]amino]benzamide	248140: Inhibition of FGF-stimulated human umbilical vein endothelial cell proliferation	ic50	0.0010	uM
N-[5-cyano-4-[[(1R,2R)-2-methoxycyclopentyl]amino]-2-pyridinyl]-7-formyl-6-[(3-oxomorpholin-4-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1542819: Inhibition of FGFR4 (unknown origin) incubated for 60 mins by caliper microfluidic mobility shift technology based assay	ic50	0.0010	uM
N-[5-cyano-4-[[(3R)-oxolan-3-yl]amino]-2-pyridinyl]-7-formyl-6-[[(3R)-3-methoxy-2-oxopyrrolidin-1-yl]methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1542819: Inhibition of FGFR4 (unknown origin) incubated for 60 mins by caliper microfluidic mobility shift technology based assay	ic50	0.0010	uM
N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-5-[2-[ethyl(propyl)amino]ethyl]-3-methylphenyl]prop-2-enamide	1773781: Inhibition of N-terminal GST fusion tagged human FGFR4 cytoplasmic domain (460 to 802 end residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate addition and further incubated for 30 mins in presence of ATP at Km concentration by caliper mobility shift assay	ic50	0.0010	uM
N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-3-methyl-5-[2-[2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]ethyl]phenyl]prop-2-enamide	1773781: Inhibition of N-terminal GST fusion tagged human FGFR4 cytoplasmic domain (460 to 802 end residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate addition and further incubated for 30 mins in presence of ATP at Km concentration by caliper mobility shift assay	ic50	0.0010	uM
1-tert-butyl-3-[3-(3,5-dimethoxyphenyl)-7-(3-morpholin-4-ylpropylamino)-1,6-naphthyridin-2-yl]urea	248925: Inhibition of FGF-stimulated human umbilical vein endothelial cell proliferation	ic50	0.0010	uM
1-tert-butyl-3-[3-(3,5-dimethoxyphenyl)-7-[3-(4-methylpiperazin-1-yl)propylamino]-1,6-naphthyridin-2-yl]urea	248925: Inhibition of FGF-stimulated human umbilical vein endothelial cell proliferation	ic50	0.0010	uM
6-[[acetyl(propan-2-yl)amino]methyl]-N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide	1717930: Inhibition of recombinant non-phosphorylated FGFR4 kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay	ic50	0.0011	uM
N-(5-cyano-4-propan-2-yloxy-2-pyridinyl)-6-formyl-2,3-dihydropyrrolo[2,3-b]pyridine-1-carboxamide	1409769: Inhibition of FGFR4 (388 to 802 residues) (unknown origin) using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 as substrate after 60 mins by microfluidic mobility shift assay	ic50	0.0011	uM
N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-3-methyl-5-[2-[4-(oxetan-3-yl)piperazin-1-yl]ethyl]phenyl]prop-2-enamide	1773781: Inhibition of N-terminal GST fusion tagged human FGFR4 cytoplasmic domain (460 to 802 end residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate addition and further incubated for 30 mins in presence of ATP at Km concentration by caliper mobility shift assay	ic50	0.0011	uM
N-[2-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]-5-[2-[4-(2-methoxyethyl)piperazin-1-yl]ethyl]-3-methylphenyl]prop-2-enamide	1773781: Inhibition of N-terminal GST fusion tagged human FGFR4 cytoplasmic domain (460 to 802 end residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate addition and further incubated for 30 mins in presence of ATP at Km concentration by caliper mobility shift assay	ic50	0.0011	uM
N-[4-[[6-(1-benzothiophen-2-yl)purin-9-yl]methyl]phenyl]prop-2-enamide	2063027: Inhibition of FGFR4 (unknown origin) by ELISA	ic50	0.0011	uM
N-[2-[[6-[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl-methylamino]pyrimidin-4-yl]amino]-5-(4-ethylpiperazin-1-yl)phenyl]prop-2-enamide	1601527: Inhibition of human FGFR4 using Poly [E,Y] 4:1 substrate pre-incubated for 15 to 60 mins followed by ATP and [gamma33P]-ATP addition	ic50	0.0012	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression	4
Heparin	affects binding, increases reaction	3
Cyclosporine	decreases expression	3
futibatinib	decreases activity	2
PD 173074	decreases reaction, increases phosphorylation, decreases activity	2
ponatinib	decreases activity	2
Air Pollutants	decreases expression, decreases methylation, increases abundance, increases expression	2
Chelating Agents	affects binding, decreases expression	2
Copper	affects binding, decreases expression	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Aflatoxin B1	affects expression, decreases methylation	2
Particulate Matter	decreases methylation, increases abundance, increases expression, affects expression	2
pirinixic acid	affects binding, decreases expression, increases activity	1
bisphenol A	affects expression	1
deoxynivalenol	decreases expression	1
beta-lapachone	decreases expression	1
sodium arsenite	increases expression	1
perfluorooctanoic acid	decreases expression	1
sulindac sulfide	decreases expression	1
periodate-oxidized adenosine	affects expression	1
coumarin	increases phosphorylation	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
obeticholic acid	decreases expression	1
abrine	decreases expression	1
Grape Seed Proanthocyanidins	affects cotreatment, increases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
MT19c compound	decreases expression	1
Zoledronic Acid	decreases expression	1
Bile Acids and Salts	decreases chemical synthesis	1
Cadmium	decreases expression, increases abundance	1

ChEMBL screening assays

900 unique, capped per target: 891 binding, 9 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1249398	Binding	Inhibition of FGFR signaling-induced STAT3 tyr705 phosphorylation in human U2OS cells at 50 nM by immunoblot analysis	A functional genomics approach to the mode of action of apratoxin A. — Nat Chem Biol
CHEMBL678499	Functional	Inhibition of fibroblast growth factor receptor(FGFR)	Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors. — J Med Chem

Cellosaurus cell lines

9 cell lines: 9 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1DH	Abcam HCT 116 FGFR4 KO 1	Cancer cell line	Male
CVCL_B8AP	Abcam HCT 116 FGFR4 KO 2	Cancer cell line	Male
CVCL_B8VV	Abcam MCF-7 FGFR4 KO	Cancer cell line	Female
CVCL_B9I9	Abcam A-549 FGFR4 KO	Cancer cell line	Male
CVCL_E0D2	Ubigene HeLa FGFR4 KO	Cancer cell line	Female
CVCL_E6ZX	MCF7-FGFR4	Cancer cell line	Female
CVCL_E6ZZ	U2OS-FGFR4	Cancer cell line	Female
CVCL_S640	RMS559	Cancer cell line	Male
CVCL_SN54	HAP1 FGFR4 (-)	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT02166463	PHASE3	ACTIVE_NOT_RECRUITING	Brentuximab Vedotin and Combination Chemotherapy in Treating Children and Young Adults With Stage IIB, Stage IIIB, IVA, or IVB Hodgkin Lymphoma
NCT02661503	PHASE3	ACTIVE_NOT_RECRUITING	HD21 for Advanced Stages
NCT02684708	PHASE3	COMPLETED	Second International Inter-Group Study for Classical Hodgkin Lymphoma in Children and Adolescents
NCT03907488	PHASE3	ACTIVE_NOT_RECRUITING	Immunotherapy (Nivolumab or Brentuximab Vedotin) Plus Combination Chemotherapy in Treating Patients With Newly Diagnosed Stage III-IV Classic Hodgkin Lymphoma
NCT04342936	PHASE3	UNKNOWN	Study of Camrelizumab (SHR-1210) vs. Chemotherapy in Participants With Relapsed or Refractory Classical Hodgkin Lymphoma
NCT04486391	PHASE3	TERMINATED	Tislelizumab Monotherapy Versus Salvage Chemotherapy for Relapsed/Refractory Classical Hodgkin Lymphoma
NCT05518318	PHASE3	UNKNOWN	GLS-010 Monotherapy Versus Chemotherapy in Patients With Relapsed or Refractory Classical Hodgkin’s Lymphoma (R/R cHL)
NCT05711628	PHASE3	WITHDRAWN	A Trial Comparing Chemotherapy Versus Novel Immune Checkpoint Inhibitor (Pembrolizumab) Plus Chemotherapy in Treating Relapsed/Refractory Classical Hodgkin Lymphoma
NCT06465446	PHASE3	NOT_YET_RECRUITING	A Study of IMM01 Plus Tiselizumab Versus Physician’s Choice Chemotherapy in PD(L)1-refractory Classical Hodgkin Lymphoma
NCT00654732	PHASE2	COMPLETED	Combination Chemotherapy With or Without Rituximab in Treating Participants With Stage III-IV Classic Hodgkin Lymphoma
NCT00742027	PHASE2	COMPLETED	Phase II Study of Oral Panobinostat in Adult Participants With Relapsed/Refractory Classical Hodgkin’s Lymphoma
NCT00967369	PHASE2	COMPLETED	Combination Chemotherapy With or Without Bortezomib in Treating Patients With Classical Hodgkin Lymphoma That Has Returned or Does Not Respond to Prior Treatment.
NCT02164500	PHASE2	COMPLETED	JAK-inhibition in Recurrent Classical Hodgkin Lymphoma
NCT02414568	PHASE2	COMPLETED	Bendamustine Study in Classical Hodgkin Lymphoma Patients Over 60 Treated by Prednisone, Vinblastine and Doxorubicin
NCT02758717	PHASE2	ACTIVE_NOT_RECRUITING	Nivolumab and Brentuximab Vedotin in Treating Older Patients With Untreated Hodgkin Lymphoma
NCT02824029	PHASE2	COMPLETED	Ibrutinib in Treating Patients With Relapsed or Refractory Classical Hodgkin Lymphoma
NCT02940301	PHASE2	ACTIVE_NOT_RECRUITING	Ibrutinib and Nivolumab in Treating Patients With Relapsed or Refractory Classical Hodgkin Lymphoma
NCT03004833	PHASE2	COMPLETED	Nivolumab and AVD in Early-stage Unfavorable Classical Hodgkin Lymphoma
NCT03057795	PHASE2	ACTIVE_NOT_RECRUITING	Nivolumab & Brentuximab Vedotin Consolidation After Autologous SCT in Patients With High-Risk Classical Hodgkin Lymphoma
NCT03209973	PHASE2	COMPLETED	A Study of Tislelizumab as Monotherapy in Relapsed or Refractory Classical Hodgkin Lymphoma
NCT03226249	PHASE2	UNKNOWN	PET-Directed Therapy With Pembrolizumab and Combination Chemotherapy in Treating Patients With Previously Untreated Classical Hodgkin Lymphoma
NCT03233347	PHASE2	ACTIVE_NOT_RECRUITING	Doxorubicin, Vinblastine, Dacarbazine, Brentuximab Vedotin, and Nivolumab in Treating Patients With Stage I-II Hodgkin Lymphoma
NCT03480334	PHASE2	ACTIVE_NOT_RECRUITING	Abscopal Effect of Radiotherapy and Nivolumab in Relapsed Hodgkin Lymphoma After Anti-PD1 Therapy
NCT03527628	PHASE2	UNKNOWN	OPTmizing Advanced Stage HodgkIn LymphoMa patIentS Therapy
NCT03580564	PHASE2	COMPLETED	An Open, Multicenter Phase II Study to Evaluate the Safety and Efficacy of KL-A167 Injection in Relapsed or Refractory Classical Hodgkin’s Lymphoma
NCT03652441	PHASE2	COMPLETED	Consolidation Therapy With Brentuximab Vedotin After Allogeneic Stem Cell Transplantation for Relapsed or Refractory Hodgkin Lymphoma
NCT03655483	PHASE2	UNKNOWN	Study of GLS-010 Injection in the Treatment of Classical Hodgkin’s Lymphoma
NCT03712202	PHASE2	ACTIVE_NOT_RECRUITING	Brentuximab Vedotin and Nivolumab in Treating Patients With Early Stage Classic Hodgkin Lymphoma
NCT04067037	PHASE2	ACTIVE_NOT_RECRUITING	Camrelizumab Combined With AVD in the First-line Treatment for Patients With Advanced Classical Hodgkin’s Lymphoma
NCT04318080	PHASE2	COMPLETED	Tislelizumab in Participants With Relapsed or Refractory Classical Hodgkin Lymphoma
NCT04510636	PHASE2	RECRUITING	Study of Pembrolizumab With Bendamustine in Hodgkin Lymphoma
NCT04624984	PHASE2	UNKNOWN	PD-1 Inhibitor or PD-1 Inhibitor Plus GVD for Relapsed/Refractory CHL
NCT04788043	PHASE2	ACTIVE_NOT_RECRUITING	Study of Magrolimab and Pembrolizumab in Relapsed or Refractory Classic Hodgkin Lymphoma
NCT04837859	PHASE2	RECRUITING	Phase II Trial of Individualized Immunotherapy in Early-Stage Unfavorable Classical Hodgkin Lymphoma
NCT04838652	PHASE2	RECRUITING	Pembrolizumab in Combination With Salvage Chemotherapy for First-relapsed or Refractory Classical Hodgkin Lymphoma
NCT05008224	PHASE2	COMPLETED	Study of Safety and Efficacy of Pembrolizumab and Chemotherapy in Participants With Newly Diagnosed Classical Hodgkin Lymphoma (cHL) (MK-3475-C11/KEYNOTE-C11)
NCT05039073	PHASE2	RECRUITING	Brentuximab Vedotin and Nivolumab for the Treatment of Relapsed/Refractory Classic Hodgkin Lymphoma Previously Treated With Brentuximab Vedotin or Checkpoint Inhibitors
NCT05179603	PHASE2	TERMINATED	A Study of SAR444245 With or Without Other Anticancer Therapies for the Treatment of Adults and Adolescents With Relapsed or Refractory B Cell Lymphoma (Master Protocol) [Pegathor Lymphoma 205]
NCT05404945	PHASE2	ACTIVE_NOT_RECRUITING	Fitness-adapted, Pembrolizumab-based Therapy for Untreated Classical Hodgkin Lymphoma Patients 60 Years of Age and Above
NCT05900765	PHASE2	RECRUITING	A Study of Zimberelimab(GLS-010) Combined With AVD for Newly Diagnosed Early-stage Hodgkin’s Lymphoma