FLT3

Summary

FLT3 (fms related receptor tyrosine kinase 3, HGNC:3765) is a protein-coding gene on chromosome 13q12.2, encoding Receptor-type tyrosine-protein kinase FLT3 (P36888). Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells. In precision oncology, FLT3 ITD confers sensitivity to Gilteritinib in Acute Myeloid Leukemia (CIViC Level A); 79 further curated variant–drug associations are listed below.

This gene encodes a class III receptor tyrosine kinase that regulates hematopoiesis. This receptor is activated by binding of the fms-related tyrosine kinase 3 ligand to the extracellular domain, which induces homodimer formation in the plasma membrane leading to autophosphorylation of the receptor. The activated receptor kinase subsequently phosphorylates and activates multiple cytoplasmic effector molecules in pathways involved in apoptosis, proliferation, and differentiation of hematopoietic cells in bone marrow. Mutations that result in the constitutive activation of this receptor result in acute myeloid leukemia and acute lymphoblastic leukemia.

Source: NCBI Gene 2322 — RefSeq curated summary.

At a glance

• Gene–disease (curated): leukemia, acute myeloid, susceptibility to (Limited, ClinGen)
• GWAS associations: 63
• Clinical variants (ClinVar): 245 total — 10 pathogenic, 4 likely-pathogenic
• Phenotypes (HPO): 5
• Druggable target: yes — 143 molecules with ChEMBL bioactivity
• Precision-oncology evidence (CIViC): 80 curated variant–drug associations
• Cancer driver (intOGen): activating (oncogene-like) across 2 cancer types
• Transcription factor: yes — 19 downstream targets (CollecTRI)
• MANE Select transcript: NM_004119

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:3765
Approved symbol	FLT3
Name	fms related receptor tyrosine kinase 3
Location	13q12.2
Locus type	gene with protein product
Status	Approved
Aliases	STK1, FLK2, CD135
Ensembl gene	ENSG00000122025
Ensembl biotype	protein_coding
OMIM	136351
Entrez	2322

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 2 protein_coding, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000241453, ENST00000380987, ENST00000469894, ENST00000864668

RefSeq mRNA: 1 — MANE Select: NM_004119 NM_004119

CCDS: CCDS31953

Canonical transcript exons

ENST00000241453 — 24 exons

Exon	Start	End
ENSE00000827401	28037185	28037288
ENSE00000827402	28035935	28036043
ENSE00000827403	28035495	28035673
ENSE00000827404	28034301	28034407
ENSE00000827405	28034082	28034214
ENSE00000827406	28033887	28033991
ENSE00000827407	28028178	28028288
ENSE00000827408	28027088	28027241
ENSE00000906608	28048275	28048443
ENSE00000906609	28049384	28049537
ENSE00000906610	28049635	28049774
ENSE00000906611	28050095	28050222
ENSE00000906612	28052545	28052674
ENSE00000906613	28057347	28057462
ENSE00000906614	28061867	28062069
ENSE00000906615	28070491	28070612
ENSE00001487116	28003274	28004174
ENSE00003513156	28014452	28014557
ENSE00003519436	28023350	28023477
ENSE00003552851	28015590	28015701
ENSE00003565636	28024861	28024943
ENSE00003598146	28018467	28018589
ENSE00003692016	28015157	28015256
ENSE00003896396	28100468	28100576

Expression profiles

Bgee: expression breadth ubiquitous, 166 present calls, max score 86.25.

FANTOM5 (CAGE): breadth broad, TPM avg 2.7806 / max 577.0111, expressed in 297 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
136527	2.7297	296
136526	0.0509	21

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	86.25	gold quality
cerebellar hemisphere	UBERON:0002245	81.49	gold quality
cerebellar cortex	UBERON:0002129	81.37	gold quality
monocyte	CL:0000576	81.07	gold quality
mononuclear cell	CL:0000842	80.55	gold quality
leukocyte	CL:0000738	80.03	gold quality
right hemisphere of cerebellum	UBERON:0014890	80.01	gold quality
cerebellum	UBERON:0002037	79.31	gold quality
bone marrow cell	CL:0002092	73.72	silver quality
bone marrow	UBERON:0002371	72.76	gold quality
lymph node	UBERON:0000029	71.18	gold quality
granulocyte	CL:0000094	70.09	gold quality
body of pancreas	UBERON:0001150	69.61	gold quality
spleen	UBERON:0002106	68.87	gold quality
vermiform appendix	UBERON:0001154	68.31	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	67.90	gold quality
gall bladder	UBERON:0002110	66.94	gold quality
pancreas	UBERON:0001264	66.82	gold quality
right lung	UBERON:0002167	66.38	gold quality
blood	UBERON:0000178	66.37	gold quality
pigmented layer of retina	UBERON:0001782	66.30	gold quality
spinal cord	UBERON:0002240	65.24	gold quality
caecum	UBERON:0001153	63.82	gold quality
cerebellar vermis	UBERON:0004720	63.55	silver quality
tibialis anterior	UBERON:0001385	63.36	silver quality
islet of Langerhans	UBERON:0000006	62.86	gold quality
rectum	UBERON:0001052	62.02	gold quality
prefrontal cortex	UBERON:0000451	61.12	gold quality
small intestine Peyer’s patch	UBERON:0003454	61.08	gold quality
epithelial cell of pancreas	CL:0000083	59.89	gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-MTAB-6678	yes	171.14
E-HCAD-6	yes	29.00
E-ANND-3	yes	10.72
E-MTAB-9801	yes	8.15
E-GEOD-99795	no	21.87

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

19 targets.

Target	Regulation
BCL2L1	Activation
BCL2L11	Repression
CDKN1A	Activation
CDKN1B	Repression
CEBPA	Unknown
CEBPB	Repression
CISH	Activation
FZD4	Unknown
ID1	Activation
PARP1	Activation
PIM1	Activation
PIM2	Activation
PTPN6	Unknown
RAD51	Activation
SOCS2	Activation
SOCS3	Activation
SPI1	Unknown
USP22	Activation
XRCC5	Activation

Upstream regulators (CollecTRI, top): CEBPA, HES1, HOXA9, IKZF1, KAT6B, MEIS1, MYB, NCOR1, PAX5, PML, RUNX1, SPI1, STAT3, TXK

miRNA regulators (miRDB)

56 targeting FLT3, 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-4533	100.00	69.48	2758
HSA-MIR-518D-5P	100.00	67.51	979
HSA-MIR-518E-5P	100.00	67.66	954
HSA-MIR-518F-5P	100.00	67.51	979
HSA-MIR-519A-5P	100.00	67.66	954
HSA-MIR-519B-5P	100.00	67.66	954
HSA-MIR-519C-5P	100.00	67.66	954
HSA-MIR-520C-5P	100.00	67.51	979
HSA-MIR-522-5P	100.00	67.66	954
HSA-MIR-523-5P	100.00	67.66	954
HSA-MIR-526A-5P	100.00	67.51	979
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-6798-5P	100.00	65.77	699
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-520G-5P	99.99	66.76	658
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-570-3P	99.96	72.41	4910
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-4493	99.90	66.48	977
HSA-MIR-424-5P	99.89	71.90	2641
HSA-MIR-6838-5P	99.89	71.94	2690
HSA-MIR-3140-3P	99.88	68.47	2069
HSA-MIR-4698	99.84	71.41	4303
HSA-MIR-139-5P	99.80	69.50	1399

Literature-anchored findings (GeneRIF, showing 40)

• First report of D835X mutations in human. Activating mutation of D835 within the activation loop of FLT3 in human hematologic malignancies. (PMID:11290608)
• Flt3/Flk-2-ligand in synergy with thrombopoietin may slow down megakaryocyte development by causing increased proliferation of megakaryocyte progenitor cells. (PMID:11983110)
• induces acute promyelocytic leukemia in a mouse model (PMID:12060771)
• Analysis of FLT3 length mutations in 1003 patients with acute myeloid leukemia (PMID:12070009)
• duplicated in relapsed acute myeloid leukemia (PMID:12239146)
• mutations occur in paired presentation and relapse samples from patients with acute myeloid leukemia (PMID:12239147)
• 767 of 6586 genes differed in expression between FLT3-WT- and FLT-ITD(internal tandem duplication)-expressing cell lines. ITD mutations of Flt3 activate transcriptional programs that partially mimic IL-3 activity. (PMID:12468433)
• Internal tandem duplication of the Flt3 gene appearing or altering at time of AML relapse suggests Flt3-gene abnormalities are very important in the pathogenesis of chemotherapy-resistant AML (PMID:12481903)
• The striking difference in flt3 and c-kit expression on hematopoietic stem cells translated into a corresponding difference in flt3 and c-kit function because FL was more efficient than SCF at supporting the survival of HSCs (PMID:12676789)
• Intracellular signaling initiated by Flt3 ligation modulates the functional phenotype for native human AML blasts both with and without genetic Flt3 abnormalities. (PMID:12681969)
• FLT3 mutations that lead to constitutive receptor activation and confer a poor prognosis in AML (PMID:12691136)
• FLT3/ITD is less common in pediatric than in adult acute myeloid leukemia and FLT3/ITD is a strong and independent adverse prognostic factor, and high ratios between mutant and WT-FLT3 further compromise prognosis. (PMID:12816873)
• antiapoptotic pathways from FLT3 with internal tandem duplication are more divergent than those from WtFLT3 (PMID:12842996)
• Mutations in the FLT3 gene are common in AML, including tandem repeats or a mutation in the kinase domain. (PMID:12854887)
• No significant correlation was found between FLT3 mutations and high levels of MDR1 in acute myeloid leukemia. (PMID:12926083)
• REVIEW: The role of FLT3 mutations in APL and other AML (PMID:12935959)
• wtFLT3 is often constitutively activated by FLT3 ligand in AML and thus, like its mutated form, might contribute to the altered signaling that characterizes leukemogenesis. (PMID:12969963)
• FLT3-D835/I836 mutations are one of the second genetic events in infant ALL with MLL rearrangements or pediatric ALL with hyperdiploidy (PMID:14504097)
• reduced AML1 activities predispose cells to the acquisition of the activating FLT3 mutation as a secondary event leading to full transformation in acute myeloblastic leukemia M0 (PMID:14562119)
• distinct activating FLT3-TKD mutations at position D835 mediate primary resistance to FLT3 PTK inhibitors in FLT3-transformed cell lines (PMID:14604974)
• FLT3 mutations are associated with molecular lesions in acute myeloid leukemias (PMID:14630076)
• Phosphorylation is inhibited by SU11248 in acute myeloid leukemia. (PMID:14654525)
• search for the presence of FLT3 mutations in leukemic blasts from 71 patients with childhood acute lymphoblastic leukemia discovered three novel in-frame deletions within a 7-amino acid region of the receptor juxtamembrane domain. (PMID:14670924)
• FLT3 analysis shows the autoinhibitory conformation of its complete juxtamembrane domain (PMID:14759363)
• FLT3 Asp(835) mutations may have a role in relapse of acute myeloid leukemia (PMID:14977832)
• FLT3 can negatively regulate Foxo transcription factors, thereby promoting cell survival and proliferation. (PMID:14981546)
• Mutations of Flt3 may disrupt transcriptional repressor function resulting in aberrant gene regulation and abnormal leukemia cell growth. (PMID:14982881)
• Activating mutations in the FLT3 RTK gene were found in each of 3 CD117/KIT(+) cases that were analyzed, but not in 52 other adult T-acute lymphoblastic leukemia (PMID:15044257)
• CXCR-4 expression was significantly higher in fetal liver tyrosine kinase-3 (Flt3)/internal tandem duplication (ITD) acute myeloid leukemia (PMID:15054042)
• Internal tandem duplication of the juxtamembrane domain or by activating point mutations in the second tyrosine kinase domain in FLT3 are associated with leukocytosis and the monocytic FAB subtypes M4 and M5. (PMID:15059064)
• Flt3 mutations identify patients at high risk of relapse (PMID:15061200)
• FLT3/internal tandem duplication(ITD) mutations confer a particularly poor prognosis in pediatric acute myelogenous leukemia patients (PMID:15166029)
• high frequency of FLT3 mutations in adult acute myelocytic leukemia without recurrent cytogenetic translocations. (PMID:15167911)
• FLT3 autoinhibited structure showed that N841 is the key residue in a hydrogen-bonding network that likely stabilizes the activation loop (PMID:15178581)
• Wild-type Flt3-overexpressing CD34+ cells exposed to high levels of its physiologic ligand did not produce early cobblestone areas (PMID:15242879)
• FLT3 has roles in different signal transduction pathways that control proliferation, survival and other processes in hematopoietic cells [review] (PMID:15253381)
• The loss of a clone with a mutation in the FLT3 gene at relapse did not improve the prognosis. (PMID:15289019)
• Inspection of the FLT3 structure revealed that Y842 is the key residue in regulating the switch from the closed to the open (= active) conformation of the FLT3 activation loop (PMID:15345593)
• mutations of specific residues located in the activation loop (D835X and 836-deletion in Flt-3; D816V in c-Kit) as well as a 6-base pair (6-bp) insertion at residue 840 in Flt-3 operate in a similar way (PMID:15363457)
• transformation of TF-1 cells with FLT3/ITD mutations suppressed the activity of SHP-1 by approximately 3-fold (PMID:15574429)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Flt3	ENSMUSG00000042817
rattus_norvegicus	Flt3	ENSRNOG00000054764

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), 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), FGFR4 (ENSG00000160867), DDR2 (ENSG00000162733), RYK (ENSG00000163785), MST1R (ENSG00000164078), LMTK2 (ENSG00000164715)

Protein

Protein identifiers

Receptor-type tyrosine-protein kinase FLT3 — P36888 (reviewed: P36888)

Alternative names: FL cytokine receptor, Fetal liver kinase-2, Fms-like tyrosine kinase 3, Stem cell tyrosine kinase 1

All UniProt accessions (2): E7ER61, P36888

UniProt curated annotations — full annotation on UniProt →

Function. Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells. Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation of FES, FER, PTPN6/SHP, PTPN11/SHP-2, PLCG1, and STAT5A and/or STAT5B. Activation of wild-type FLT3 causes only marginal activation of STAT5A or STAT5B. Mutations that cause constitutive kinase activity promote cell proliferation and resistance to apoptosis via the activation of multiple signaling pathways.

Subunit / interactions. Monomer in the absence of bound FLT3LG. Homodimer in the presence of bound FLT3LG. Interacts with FIZ1 following ligand activation. Interacts with FES, FER, LYN, FGR, HCK, SRC and GRB2. Interacts with PTPRJ/DEP-1 and PTPN11/SHP2. Interacts with RNF115 and RNF126. (Microbial infection) Interacts with human cytomegalovirus protein UL7.

Subcellular location. Membrane. Endoplasmic reticulum lumen.

Tissue specificity. Detected in bone marrow, in hematopoietic stem cells, in myeloid progenitor cells and in granulocyte/macrophage progenitor cells (at protein level). Detected in bone marrow, liver, thymus, spleen and lymph node, and at low levels in kidney and pancreas. Highly expressed in T-cell leukemia.

Post-translational modifications. N-glycosylated, contains complex N-glycans with sialic acid. Autophosphorylated on several tyrosine residues in response to FLT3LG binding. FLT3LG binding also increases phosphorylation of mutant kinases that are constitutively activated. Dephosphorylated by PTPRJ/DEP-1, PTPN1, PTPN6/SHP-1, and to a lesser degree by PTPN12. Dephosphorylation is important for export from the endoplasmic reticulum and location at the cell membrane. Rapidly ubiquitinated by UBE2L6 and the E3 ubiquitin-protein ligase SIAH1 after autophosphorylation, leading to its proteasomal degradation.

Disease relevance. Leukemia, acute myelogenous (AML) [MIM:601626] A subtype of acute leukemia, a cancer of the white blood cells. AML is a malignant disease of bone marrow characterized by maturational arrest of hematopoietic precursors at an early stage of development. Clonal expansion of myeloid blasts occurs in bone marrow, blood, and other tissue. Myelogenous leukemias develop from changes in cells that normally produce neutrophils, basophils, eosinophils and monocytes. The gene represented in this entry may be involved in disease pathogenesis. Somatic mutations that lead to constitutive activation of FLT3 are frequent in AML patients. These mutations fall into two classes, the most common being in-frame internal tandem duplications of variable length in the juxtamembrane region that disrupt the normal regulation of the kinase activity. Likewise, point mutations in the activation loop of the kinase domain can result in a constitutively activated kinase.

Activity regulation. Present in an inactive conformation in the absence of bound ligand. FLT3LG binding leads to dimerization and activation by autophosphorylation.

Domain organisation. The juxtamembrane autoregulatory region is important for normal regulation of the kinase activity and for maintaining the kinase in an inactive state in the absence of bound ligand. Upon tyrosine phosphorylation, it mediates interaction with the SH2 domains of numerous signaling partners. In-frame internal tandem duplications (ITDs) result in constitutive activation of the kinase. The activity of the mutant kinase can be stimulated further by FLT3LG binding.

Miscellaneous. Can be used as diagnostic tool to establish the exact cause of acute myeloid leukemia, and to determine the optimal therapy.

Similarity. Belongs to the protein kinase superfamily. Tyr protein kinase family. CSF-1/PDGF receptor subfamily.

Isoforms (2)

UniProt ID	Names	Canonical?
P36888-1	1	yes
P36888-2	2

RefSeq proteins (1): NP_004110* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR001245	Ser-Thr/Tyr_kinase_cat_dom	Domain
IPR001824	Tyr_kinase_rcpt_3_CS	Conserved_site
IPR007110	Ig-like_dom	Domain
IPR008266	Tyr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR013151	Immunoglobulin_dom	Domain
IPR013783	Ig-like_fold	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR020635	Tyr_kinase_cat_dom	Domain
IPR036179	Ig-like_dom_sf	Homologous_superfamily
IPR050122	RTK	Family

Pfam: PF00047, PF07714

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 (100 total): helix 16, strand 15, sequence variant 14, modified residue 13, glycosylation site 10, disulfide bond 7, sequence conflict 6, mutagenesis site 4, turn 3, binding site 2, topological domain 2, domain 2, signal peptide 1, chain 1, transmembrane region 1, splice variant 1, region of interest 1, active site 1

Structure

Experimental structures (PDB)

11 structures.

PDB	Method	Resolution (Å)
1RJB	X-RAY DIFFRACTION	2.1
6JQR	X-RAY DIFFRACTION	2.2
5X02	X-RAY DIFFRACTION	2.4
6IL3	X-RAY DIFFRACTION	2.5
8XB1	X-RAY DIFFRACTION	2.85
4RT7	X-RAY DIFFRACTION	3.1
4XUF	X-RAY DIFFRACTION	3.2
7QDP	X-RAY DIFFRACTION	3.69
3QS7	X-RAY DIFFRACTION	4.3
7ZV9	X-RAY DIFFRACTION	4.51
3QS9	X-RAY DIFFRACTION	7.8

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P36888-F1	76.19	0.30

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): 811 (proton acceptor)

Ligand- & substrate-binding residues (2): 644; 616–624

Post-translational modifications (13): 572, 574, 589, 591, 599, 726, 759, 768, 793, 842, 955, 969, 993

Disulfide bonds (7): 35–65, 103–114, 199–206, 232–241, 272–330, 368–407, 381–392

Glycosylation sites (10): 43, 100, 151, 306, 323, 351, 354, 473, 502, 541

Mutagenesis-validated functional residues (4):

Position	Phenotype
589	reduced phosphorylation of the wild-type kinase in response to ligand binding. no effect on the phosphorylation of the c
591	no significant effect on tyrosine phosphorylation. abolishes activation of stat5a.
599	abolishes interaction with ptpn11/shp2 and phosphorylation of ptpn11/shp2.
644	abolishes kinase activity.

Function

Pathways and Gene Ontology

Reactome pathways

27 pathways

ID	Pathway
R-HSA-109704	PI3K Cascade
R-HSA-1257604	PIP3 activates AKT signaling
R-HSA-2219530	Constitutive Signaling by Aberrant PI3K in Cancer
R-HSA-5673001	RAF/MAP kinase cascade
R-HSA-6811558	PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling
R-HSA-9607240	FLT3 Signaling
R-HSA-9645135	STAT5 Activation
R-HSA-9702509	FLT3 mutants bind TKIs
R-HSA-9702518	STAT5 activation downstream of FLT3 ITD mutants
R-HSA-9702569	KW2449-resistant FLT3 mutants
R-HSA-9702577	semaxanib-resistant FLT3 mutants
R-HSA-9702581	crenolanib-resistant FLT3 mutants
R-HSA-9702590	gilteritinib-resistant FLT3 mutants
R-HSA-9702596	lestaurtinib-resistant FLT3 mutants
R-HSA-9702600	midostaurin-resistant FLT3 mutants
R-HSA-9702605	pexidartinib-resistant FLT3 mutants
R-HSA-9702614	ponatinib-resistant FLT3 mutants
R-HSA-9702620	quizartinib-resistant FLT3 mutants
R-HSA-9702624	sorafenib-resistant FLT3 mutants
R-HSA-9702632	sunitinib-resistant FLT3 mutants
R-HSA-9702636	tandutinib-resistant FLT3 mutants
R-HSA-9702998	linifanib-resistant FLT3 mutants
R-HSA-9703009	tamatinib-resistant FLT3 mutants
R-HSA-9703648	Signaling by FLT3 ITD and TKD mutants
R-HSA-9706369	Negative regulation of FLT3
R-HSA-9706374	FLT3 signaling through SRC family kinases
R-HSA-9706377	FLT3 signaling by CBL mutants

MSigDB gene sets: 0 (showing top):

GO Biological Process (26): leukocyte homeostasis (GO:0001776), myeloid progenitor cell differentiation (GO:0002318), pro-B cell differentiation (GO:0002328), cell surface receptor protein tyrosine kinase signaling pathway (GO:0007169), positive regulation of cell population proliferation (GO:0008284), cell migration (GO:0016477), peptidyl-tyrosine phosphorylation (GO:0018108), cytokine-mediated signaling pathway (GO:0019221), hemopoiesis (GO:0030097), B cell differentiation (GO:0030183), common myeloid progenitor cell proliferation (GO:0035726), positive regulation of tyrosine phosphorylation of STAT protein (GO:0042531), regulation of apoptotic process (GO:0042981), positive regulation of MAP kinase activity (GO:0043406), positive regulation of MAPK cascade (GO:0043410), lymphocyte proliferation (GO:0046651), protein autophosphorylation (GO:0046777), positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051897), cellular response to cytokine stimulus (GO:0071345), cellular response to glucocorticoid stimulus (GO:0071385), dendritic cell differentiation (GO:0097028), liver regeneration (GO:0097421), protein phosphorylation (GO:0006468), cell surface receptor signaling pathway (GO:0007166), positive regulation of macromolecule metabolic process (GO:0010604), vascular endothelial growth factor signaling pathway (GO:0038084)

GO Molecular Function (15): protein tyrosine kinase activity (GO:0004713), transmembrane receptor protein tyrosine kinase activity (GO:0004714), cytokine receptor activity (GO:0004896), vascular endothelial growth factor receptor activity (GO:0005021), ATP binding (GO:0005524), growth factor binding (GO:0019838), nuclear glucocorticoid receptor binding (GO:0035259), protein-containing complex binding (GO:0044877), phosphatidylinositol 3-kinase activator activity (GO:0141038), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), transmembrane signaling receptor activity (GO:0004888), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (7): endoplasmic reticulum (GO:0005783), endoplasmic reticulum lumen (GO:0005788), plasma membrane (GO:0005886), endosome membrane (GO:0010008), signaling receptor complex (GO:0043235), membrane (GO:0016020), protein-containing complex (GO:0032991)

Reactome top-level categories

Rollup of top-10 pathways:

Category	Pathways
Drug resistance of FLT3 mutants	11
IRS-mediated signalling	1
Intracellular signaling by second messengers	1
PI3K/AKT Signaling in Cancer	1
MAPK1/MAPK3 signaling	1
Negative regulation of the PI3K/AKT network	1
Cytokine Signaling in Immune system	1
FLT3 Signaling	1
FLT3 signaling in disease	1
Signaling by FLT3 ITD and TKD mutants	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cell population proliferation	2
protein phosphorylation	2
positive regulation of intracellular signal transduction	2
binding	2
immune system process	1
homeostasis of number of cells	1
hematopoietic progenitor cell differentiation	1
lymphoid progenitor cell differentiation	1
enzyme-linked receptor protein signaling pathway	1
regulation of cell population proliferation	1
positive regulation of cellular process	1
cell motility	1
peptidyl-tyrosine modification	1
cell surface receptor signaling pathway	1
cellular response to cytokine stimulus	1
cell development	1
lymphocyte differentiation	1
B cell activation	1
tyrosine phosphorylation of STAT protein	1
regulation of tyrosine phosphorylation of STAT protein	1
positive regulation of peptidyl-tyrosine phosphorylation	1
apoptotic process	1
regulation of programmed cell death	1
MAP kinase activity	1
regulation of MAP kinase activity	1
positive regulation of MAPK cascade	1
positive regulation of protein serine/threonine kinase activity	1
MAPK cascade	1
regulation of MAPK cascade	1
mononuclear cell proliferation	1
lymphocyte activation	1
phosphatidylinositol 3-kinase/protein kinase B signal transduction	1
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	1
response to cytokine	1
response to glucocorticoid	1
cellular response to corticosteroid stimulus	1
protein kinase activity	1
protein tyrosine kinase activity	1
transmembrane receptor protein kinase activity	1
transmembrane signaling receptor activity	1

Protein interactions and networks

STRING

3157 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
FLT3	FLT3LG	P49771	998
FLT3	KITLG	P21583	953
FLT3	NPM1	P06748	935
FLT3	CD34	P28906	873
FLT3	IL3	P08700	864
FLT3	ASXL1	Q8IXJ9	861
FLT3	DNMT3A	Q9Y6K1	851
FLT3	TET2	Q6N021	850
FLT3	SLAMF1	Q13291	832
FLT3	RUNX1	Q01196	825
FLT3	IL7R	P16871	822
FLT3	IDH1	O75874	815
FLT3	CSF2	P04141	814
FLT3	CEBPA	P49715	812
FLT3	IDH2	P48735	797

IntAct

85 interactions, top by confidence:

A	B	Type	Score
SYK	FLT3	psi-mi:“MI:0407”(direct interaction)	0.740
SYK	FLT3	psi-mi:“MI:0217”(phosphorylation reaction)	0.740
FLT3	SYK	psi-mi:“MI:0915”(physical association)	0.740
SYK	FLT3	psi-mi:“MI:0914”(association)	0.740
FLT3	SYK	psi-mi:“MI:0403”(colocalization)	0.740
GRB10	FLT3	psi-mi:“MI:0915”(physical association)	0.590
FLT3	GRB10	psi-mi:“MI:0915”(physical association)	0.590
ABL2	FLT3	psi-mi:“MI:0407”(direct interaction)	0.540

BioGRID (328): FLT3 (Negative Genetic), VHL (Negative Genetic), FLT3 (Affinity Capture-MS), UBC (Affinity Capture-Western), FLT3 (Affinity Capture-MS), SPRY3 (Positive Genetic), SERPINE1 (Positive Genetic), NUAK1 (Positive Genetic), NDUFS5 (Positive Genetic), SULT1A3 (Positive Genetic), PCDHA3 (Positive Genetic), PCDHA12 (Positive Genetic), PCDHAC1 (Positive Genetic), PCDHA1 (Positive Genetic), PCDHAC2 (Positive Genetic)

ESM2 similar proteins: A0A1D5NSM8, B1AUH1, B3DK56, B3EX02, B8UU59, E2RK30, E9PZ36, E9Q612, G5E8Q8, H2A0L8, O08775, O14522, O88488, P08922, P08941, P08F94, P0C5E4, P28827, P28828, P29392, P35822, P36888, P86091, P97435, P98072, P98073, P98074, Q00342, Q05546, Q12913, Q15262, Q16827, Q26627, Q28920, Q5GIT4, Q63132, Q64455, Q6DIV5, Q6YI48, Q78DX7

Diamond homologs: D2IYS2, G3V9H8, O08775, O42127, O73791, O73798, O97799, P00529, P00545, P04048, P05532, P05622, P07333, P07949, P09581, P09619, P10721, P11362, P13369, P16092, P16234, P17948, P18460, P18461, P20786, P21802, P21803, P21804, P22182, P22455, P22607, P23049, P26618, P26619, P33497, P35546, P35590, P35916, P35917, P35918

SIGNOR signaling

115 interactions.

A	Effect	B	Mechanism
FLT3	up-regulates	FLT3	phosphorylation
sunitinib	down-regulates	FLT3	“chemical inhibition”
anthra[1,9-cd]pyrazol-6(2H)-one	down-regulates	FLT3	“chemical inhibition”
CHIR-124	down-regulates	FLT3	“chemical inhibition”
4-amino-5-fluoro-3-[5-(4-methyl-1-piperazinyl)-1,3-dihydrobenzimidazol-2-ylidene]-2-quinolinone	down-regulates	FLT3	“chemical inhibition”
“dovitinib; bis(lactic acid)”	down-regulates	FLT3	“chemical inhibition”
[4-[2-(1H-indazol-3-yl)ethenyl]phenyl]-(1-piperazinyl)methanone	down-regulates	FLT3	“chemical inhibition”
MK-2461	down-regulates	FLT3	“chemical inhibition”
FLT3	up-regulates	Skeletal_muscle_differentiation
quizartinib	down-regulates	FLT3	“chemical inhibition”
tandutinib	down-regulates	FLT3	“chemical inhibition”
TG101209	down-regulates	FLT3	“chemical inhibition”
FLT3	“up-regulates activity”	AKT
FLT3	“down-regulates quantity by repression”	CEBPA	“transcriptional regulation”
FLT3	“up-regulates activity”	SHC1	phosphorylation
FLT3	“up-regulates activity”	AKT1
FLT3	“up-regulates activity”	RUNX1
sunitinib	“down-regulates activity”	FLT3	“chemical inhibition”
regorafenib	“down-regulates activity”	FLT3	“chemical inhibition”
PIM1	“up-regulates quantity”	FLT3	phosphorylation
FLT3	“down-regulates quantity”	PTPN6	“transcriptional regulation”
FLT3	“up-regulates activity”	Glycolysis
FLT3	“up-regulates activity”	CTNNB1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 29 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
Regulation of signaling by CBL	6	156.8×	1e-10
FLT3 Signaling	8	145.7×	5e-14
Downstream signal transduction	5	100.2×	7e-08
Signaling by SCF-KIT	7	91.5×	9e-11
GPVI-mediated activation cascade	5	81.2×	2e-07
FCGR3A-mediated phagocytosis	5	49.3×	1e-06
Constitutive Signaling by Aberrant PI3K in Cancer	5	33.4×	6e-06
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	5	25.5×	2e-05

GO biological processes:

GO term	Partners	Fold	FDR
ephrin receptor signaling pathway	6	93.8×	1e-08
cellular response to transforming growth factor beta stimulus	5	62.8×	2e-06
T cell receptor signaling pathway	6	41.4×	1e-06
intracellular signal transduction	8	13.9×	4e-06

Disease & clinical

Cancer significance

From CIViC — curated cancer-variant interpretation:

FLT3 is an important cytokine receptor involved in normal hematopoiesis. Mutations in this gene are common in acute myeloid leukemia (AML) and screening for mutations in this gene has been recommended by the World Health Organization in patients with AML, particularly in cases of cytogenetically normal AML (CN-AML). FLT3 mutations commonly co-occur with mutations such as NPM1 that are associated with CN-AML and likely modulate prognostic impact. While FLT3-ITD mutations have been associated with poorer prognosis in AML, the prognostic impact of FLT3-TKD mutations are still up for debate.

From intOGen — cancer-driver classification: activating (oncogene-like) across 2 cancer types — ALL, AML.

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	10
Likely pathogenic	4
Uncertain significance	78
Likely benign	40
Benign	85

Top pathogenic / likely-pathogenic (14)

Variant ID	HGVS	Classification
16270	FLT3, INTERNAL TANDEM DUP	Pathogenic
16271	NM_004119.3(FLT3):c.2520_2521insGGATCC (p.Ser840_Asn841insGlySer)	Pathogenic
16272	NM_004119.3(FLT3):c.2504A>T (p.Asp835Val)	Pathogenic
16273	NM_004119.3(FLT3):c.2503G>C (p.Asp835His)	Pathogenic
16274	NM_004119.3(FLT3):c.2503G>A (p.Asp835Asn)	Pathogenic
16276	NM_004119.3(FLT3):c.2503G>T (p.Asp835Tyr)	Pathogenic
16277	NM_004119.3(FLT3):c.2503_2505del (p.Asp835del)	Pathogenic
16278	NM_004119.3(FLT3):c.1777_1779del (p.Asp593del)	Pathogenic
219096	NM_004119.3(FLT3):c.1773_1793dup (p.Tyr597_Glu598insAspValAspPheArgGluTyr)	Pathogenic
375972	NM_004119.3(FLT3):c.2505T>A (p.Asp835Glu)	Pathogenic
2572500	NM_004119.3(FLT3):c.2533A>G (p.Arg845Gly)	Likely pathogenic
4528371	NM_004119.3(FLT3):c.1715A>G (p.Tyr572Cys)	Likely pathogenic
590265	t(13;17)(q12.2;q11.2)	Likely pathogenic
800354	NM_004119.3(FLT3):c.1714T>C (p.Tyr572His)	Likely pathogenic

SpliceAI

4139 predictions. Top by Δscore:

Variant	Effect	Δscore
13:28015155:A:AC	donor_gain	1.0000
13:28015156:C:CC	donor_gain	1.0000
13:28015156:CATTT:C	donor_gain	1.0000
13:28015584:ACTT:A	donor_loss	1.0000
13:28015585:CTT:C	donor_loss	1.0000
13:28015586:TTAC:T	donor_loss	1.0000
13:28015587:TACCA:T	donor_loss	1.0000
13:28015588:A:AC	donor_gain	1.0000
13:28015588:ACCAA:A	donor_loss	1.0000
13:28015589:C:CC	donor_gain	1.0000
13:28015697:CGGGC:C	acceptor_gain	1.0000
13:28015698:GGGC:G	acceptor_gain	1.0000
13:28015698:GGGCC:G	acceptor_loss	1.0000
13:28015699:GGC:G	acceptor_gain	1.0000
13:28015699:GGCC:G	acceptor_loss	1.0000
13:28015700:GC:G	acceptor_gain	1.0000
13:28015700:GCC:G	acceptor_loss	1.0000
13:28015701:CC:C	acceptor_gain	1.0000
13:28015702:C:A	acceptor_loss	1.0000
13:28015702:C:CC	acceptor_gain	1.0000
13:28015703:T:A	acceptor_loss	1.0000
13:28015714:C:CT	acceptor_gain	1.0000
13:28015714:C:T	acceptor_gain	1.0000
13:28015715:A:T	acceptor_gain	1.0000
13:28023349:CCGA:C	donor_gain	1.0000
13:28023352:A:AC	donor_gain	1.0000
13:28023353:C:CC	donor_gain	1.0000
13:28023356:AAATT:A	donor_gain	1.0000
13:28023374:T:TA	donor_gain	1.0000
13:28028172:GGTTA:G	donor_loss	1.0000

AlphaMissense

6557 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
13:28014535:A:G	W926R	1.000
13:28014535:A:T	W926R	1.000
13:28015608:A:G	W879R	1.000
13:28015608:A:T	W879R	1.000
13:28015629:A:G	W872R	1.000
13:28015629:A:T	W872R	1.000
13:28015636:A:C	S869R	1.000
13:28015636:A:T	S869R	1.000
13:28015638:T:G	S869R	1.000
13:28015681:C:A	W854C	1.000
13:28015681:C:G	W854C	1.000
13:28015683:A:G	W854R	1.000
13:28015683:A:T	W854R	1.000
13:28018522:T:A	D829V	1.000
13:28018522:T:C	D829G	1.000
13:28018522:T:G	D829A	1.000
13:28018564:C:A	R815M	1.000
13:28018564:C:G	R815T	1.000
13:28018576:T:A	D811V	1.000
13:28018576:T:G	D811A	1.000
13:28027187:A:G	L703P	1.000
13:28028246:A:G	L662P	1.000
13:28033897:T:A	K644N	1.000
13:28033897:T:G	K644N	1.000
13:28033898:T:A	K644I	1.000
13:28033901:A:T	V643D	1.000
13:28033904:G:T	A642D	1.000
13:28033943:G:T	A629D	1.000
13:28033964:C:T	G622E	1.000
13:28033966:A:C	F621L	1.000

dbSNP variants (sampled 300 via entrez): RS1000016858 (13:28073991 G>A), RS1000110668 (13:28078727 T>A), RS1000118684 (13:28067804 C>G,T), RS1000134178 (13:28079768 G>A), RS1000144711 (13:28036292 T>C), RS1000194439 (13:28006084 T>A,C), RS1000234380 (13:28032538 A>G), RS1000277067 (13:28072547 C>A,T), RS1000338328 (13:28021160 C>A,T), RS1000366438 (13:28024061 C>T), RS1000385109 (13:28044561 T>C), RS1000402186 (13:28032948 C>T), RS1000417700 (13:28088909 C>A), RS1000524703 (13:28079007 C>T), RS1000538875 (13:28037122 T>G)

Disease associations

OMIM: gene MIM:136351 | disease phenotypes: MIM:601626, MIM:254500

GenCC curated gene-disease

Disease	Classification	Inheritance
leukemia, acute myeloid, susceptibility to	Limited	Autosomal dominant

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
leukemia, acute myeloid, susceptibility to	Limited	AD

Mondo (5): acute myeloid leukemia (MONDO:0018874), acute lymphoblastic leukemia (MONDO:0004967), atypical chronic myeloid leukemia, BCR-ABL1 negative (MONDO:0004653), plasma cell myeloma (MONDO:0009693), leukemia, acute myeloid, susceptibility to (MONDO:0100173)

Orphanet (5): Acute myeloid leukemia (Orphanet:519), Acute lymphoblastic leukemia (Orphanet:513), Atypical chronic myeloid leukemia (Orphanet:98824), Multiple myeloma (Orphanet:29073), AL amyloidosis (Orphanet:85443)

HPO phenotypes

5 total (5 of 5 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0001442	Typified by somatic mosaicism
HP:0004808	Acute myeloid leukemia
HP:0006721	Acute lymphoblastic leukemia
HP:0010982	Polygenic inheritance

GWAS associations

63 associations (top):

Study	Trait	p-value
GCST002553_1	Pancreatic cancer	2.000000e-09
GCST002783_390	Body mass index	1.000000e-07
GCST002783_476	Body mass index	3.000000e-07
GCST004129_8	White blood cell count (monocyte)	8.000000e-11
GCST004608_183	Granulocyte percentage of myeloid white cells	5.000000e-12
GCST004608_184	Granulocyte percentage of myeloid white cells	2.000000e-136
GCST004609_199	Monocyte percentage of white cells	5.000000e-25
GCST004609_200	Monocyte percentage of white cells	4.000000e-188
GCST004610_134	White blood cell count	2.000000e-19
GCST004610_135	White blood cell count	5.000000e-12
GCST004613_36	Sum neutrophil eosinophil counts	2.000000e-11
GCST004614_13	Granulocyte count	7.000000e-12
GCST004620_84	Sum basophil neutrophil counts	2.000000e-12
GCST004625_130	Monocyte count	3.000000e-10
GCST004625_131	Monocyte count	3.000000e-240
GCST004625_132	Monocyte count	2.000000e-41
GCST004625_133	Monocyte count	7.000000e-12
GCST004626_121	Myeloid white cell count	8.000000e-21
GCST004626_122	Myeloid white cell count	5.000000e-16
GCST004626_123	Myeloid white cell count	1.000000e-10
GCST004629_133	Neutrophil count	7.000000e-12
GCST004632_35	Lymphocyte percentage of white cells	1.000000e-12
GCST005977_9	Monocyte count	4.000000e-15
GCST005989_25	Serum total protein levels	1.000000e-08
GCST005990_16	Non-albumin protein levels	6.000000e-09
GCST007277_18	Tourette syndrome	2.000000e-07
GCST007469_8	Rapid automatized naming of digits	8.000000e-06
GCST007932_71	Medication use (thyroid preparations)	2.000000e-26
GCST008129_78	Body mass index	1.000000e-18
GCST008479_29	Psoriasis	6.000000e-06

EFO canonical traits (18, from GWAS)

EFO ID	Trait name
EFO:0004340	body mass index
EFO:0005091	monocyte count
EFO:0007997	granulocyte percentage of myeloid white cells
EFO:0007989	monocyte percentage of leukocytes
EFO:0004833	neutrophil count
EFO:0004842	eosinophil count
EFO:0007987	granulocyte count
EFO:0005090	basophil count
EFO:0007993	lymphocyte percentage of leukocytes
EFO:0005301	reading and spelling ability
EFO:0009933	Thyroid preparation use measurement
EFO:0004614	apolipoprotein A 1 measurement
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0009819	comparative body size at age 10, self-reported
EFO:0004587	lymphocyte count
EFO:0010701	mean reticulocyte volume
EFO:0007990	neutrophil percentage of leukocytes
EFO:0007985	platelet crit

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
D015470	Leukemia, Myeloid, Acute	C04.557.337.539.275; C15.378.508.539.275
D009101	Multiple Myeloma	C04.557.595.500; C14.907.454.460; C15.378.147.780.650; C15.378.463.515.460; C20.683.515.845; C20.683.780.650

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL1974 (SINGLE PROTEIN), CHEMBL3430908 (SELECTIVITY GROUP), CHEMBL4523735 (PROTEIN-PROTEIN INTERACTION), CHEMBL4630730 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

143 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 291,138 (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
CHEMBL1173655	AFATINIB	4	15,144
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1289494	TIVOZANIB	4	4,455
CHEMBL1289926	AXITINIB	4	15,732
CHEMBL1336	SORAFENIB	4	86,060
CHEMBL180022	NERATINIB	4	9,404
CHEMBL1834657	INFIGRATINIB PHOSPHATE	4	285
CHEMBL1852688	INFIGRATINIB	4	2,209
CHEMBL1873475	IBRUTINIB	4	7,994
CHEMBL189963	PALBOCICLIB	4	13,102
CHEMBL1946170	REGORAFENIB	4	12,678
CHEMBL1983268	ENTRECTINIB	4	3,510
CHEMBL2035187	PACRITINIB	4	3,345
CHEMBL2103830	FOSTAMATINIB	4	3,841
CHEMBL2105709	QUIZARTINIB DIHYDROCHLORIDE	4	285
CHEMBL2105717	CABOZANTINIB	4	11,177
CHEMBL2403108	CERITINIB	4	8,551
CHEMBL24828	VANDETANIB	4	42,230
CHEMBL255863	NILOTINIB	4	38,627
CHEMBL288441	BOSUTINIB	4
CHEMBL3301607	FILGOTINIB	4
CHEMBL3301610	ABEMACICLIB	4
CHEMBL3301622	GILTERITINIB	4
CHEMBL3545311	BRIGATINIB	4
CHEMBL3813873	PEXIDARTINIB	4
CHEMBL4582651	PRALSETINIB	4
CHEMBL477772	PAZOPANIB	4
CHEMBL502835	NINTEDANIB	4
CHEMBL535	SUNITINIB	4

Clinical evidence (CIViC)

Drug × variant × indication: 80 predictive associations from 98 curated evidence items; also 25 prognostic, 10 oncogenic, 5 diagnostic, 1 functional.

Variant	Therapy	Indication	Effect	Level	CIViC
FLT3 ITD	Gilteritinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC A	EID12621 +2
FLT3 ITD OR FLT3 D835 OR FLT3 I836	Gilteritinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC A	EID7728
FLT3 Mutation	Midostaurin	Acute Myeloid Leukemia	Sensitivity/Response	CIViC A	EID5261
FLT3 ITD	Sorafenib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID1040 +2
FLT3 F691L	Pexidartinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID8674 +1
FLT3 ITD	Midostaurin	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID7061 +1
FLT3 ITD	Sorafenib + Hematopoietic Cell Transplantation	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID9069 +1
FLT3 Mutation	Nilotinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID5575 +1
FLT3 Amplification	Sunitinib	Colorectal Cancer	Sensitivity/Response	CIViC B	EID11667
FLT3 ITD	Lestaurtinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID297
FLT3 ITD	Pacritinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID9217
FLT3 Mutation	Gilteritinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID7283
FLT3 TKD MUTATION	Midostaurin	Acute Myeloid Leukemia	Sensitivity/Response	CIViC B	EID1295
FLT3 F691L	Quizartinib	Acute Myeloid Leukemia	Resistance	CIViC B	EID9718 +1
FLT3 D835	Quizartinib + Sorafenib	Acute Myeloid Leukemia	Resistance	CIViC B	EID1038
FLT3 D835	Sorafenib	Acute Myeloid Leukemia	Resistance	CIViC B	EID1039
FLT3 F691L	Pexidartinib	Acute Myeloid Leukemia	Resistance	CIViC B	EID9717
FLT3 ITD	Anthracycline Antineoplastic Antibiotic + Tretinoin	Acute Promyelocytic Leukemia	Resistance	CIViC B	EID1112
FLT3 ITD	Selumetinib	Acute Myeloid Leukemia	Resistance	CIViC B	EID1137
FLT3 ITD	Tretinoin	Acute Myeloid Leukemia	Resistance	CIViC B	EID127
FLT3 TKD MUTATION	Sorafenib	Acute Myeloid Leukemia	Resistance	CIViC B	EID248
FLT3 T227M	Sunitinib	Renal Cell Carcinoma	Adverse Response	CIViC B	EID1317
FLT3 D835	Sunitinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC C	EID4024 +2
FLT3 D835V	Sunitinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC C	EID4022 +2
FLT3 D835H	Sunitinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC C	EID4027 +1
FLT3 D835Y	Gilteritinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC C	EID12620 +1
FLT3 D835Y	Sorafenib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC C	EID12625 +1
FLT3 Amplification	Regorafenib Anhydrous	Colorectal Cancer	Sensitivity/Response	CIViC C	EID7102
FLT3 Amplification	Sorafenib	Colorectal Cancer	Sensitivity/Response	CIViC C	EID7103
FLT3 Overexpression	Sunitinib	B-cell Adult Acute Lymphocytic Leukemia	Sensitivity/Response	CIViC C	EID1528

+50 more predictive associations (showing top 30 by evidence level).

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

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs1933437	Toxicity	3	sunitinib	Leukopenia;Myelosuppression;Neutropenia;Thrombocytopenia

PharmGKB variants

2 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1933437	FLT3	3	6.50	1	sunitinib
rs66520040	FLT3		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: catalytic receptor — Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

Most potent curated ligand interactions (67 total), top 25:

Ligand	Action	Affinity	Parameter
gilteritinib	Inhibition	9.52	pIC50
nefextinib	Inhibition	9.47	pIC50
denfivontinib	Inhibition	9.4	pIC50
AC710	Inhibition	9.3	pKd
Gö 6976	Inhibition	9.15	pIC50
TTT-3002	Inhibition	9.14	pIC50
crenolanib	Inhibition	9.13	pKd
compound 8i [PMID: 22765894]	Inhibition	9.1	pIC50
compound 8h [PMID: 22765894]	Inhibition	9.07	pIC50
dorsomorphin	Inhibition	9.0	pIC50
dovitinib	Inhibition	9.0	pIC50
RGB-286638	Inhibition	9.0	pIC50
ilorasertib	Inhibition	9.0	pIC50
tuspetinib	Inhibition	8.96	pIC50
compound 2c [PMID: 24900538]	Inhibition	8.68	pIC50
compound 6li [Chan et al., 2022]	Inhibition	8.6	pKd
ENMD-2076	Inhibition	8.52	pIC50
compound 5e [PMID: 28580438]	Inhibition	8.44	pKd
compound 18e [PMID: 31670517]	Inhibition	8.4	pIC50
compound 34f [PMID: 37535845]	Inhibition	8.4	pIC50
linifanib	Inhibition	8.4	pIC50
URMC-099	Inhibition	8.4	pIC50
quizartinib	Inhibition	8.38	pIC50
mivavotinib	Inhibition	8.34	pIC50
AKN-028	Inhibition	8.22	pIC50

Binding affinities (BindingDB)

774 measured of 1128 human assays (1129 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
5-[(4-hydroxycyclohexyl)amino]-3-[4-(4-methylpiperazin-1-yl)anilino]-6-propan-2-ylpyrazine-2-carboxamide	IC50	0.23 nM	US-8969336: Diamino heterocyclic carboxamide compound
3-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]-5-(oxan-4-ylamino)-6-propan-2-ylpyrazine-2-carboxamide	IC50	0.29 nM	US-8969336: Diamino heterocyclic carboxamide compound
1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea	KD	0.37 nM
6-ethyl-5-[(4-hydroxycyclohexyl)amino]-3-[3-methyl-4-(4-propan-2-ylpiperazin-1-yl)anilino]pyrazine-2-carboxamide	IC50	0.37 nM	US-8969336: Diamino heterocyclic carboxamide compound
6-ethyl-5-[(4-hydroxycyclohexyl)amino]-3-[4-(4-methylpiperazin-1-yl)anilino]pyrazine-2-carboxamide	IC50	0.4 nM	US-8969336: Diamino heterocyclic carboxamide compound
3-[4-(4-methylpiperazin-1-yl)anilino]-5-(oxan-4-ylamino)-6-propan-2-ylpyrazine-2-carboxamide	IC50	0.41 nM	US-8969336: Diamino heterocyclic carboxamide compound
4-[[5-[5-[(1-adamantylmethylamino)methyl]-2-pyridinyl]-2-(butylamino)pyrimidin-4-yl]amino]cyclohexan-1-ol	IC50	0.43 nM	US-9649309: Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
3-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-(oxan-4-ylamino)-6-propan-2-ylpyrazine-2-carboxamide	IC50	0.51 nM	US-8969336: Diamino heterocyclic carboxamide compound
5-[(4-hydroxycyclohexyl)amino]-3-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]-3-(trifluoromethyl)anilino]-6-propan-2-ylpyrazine-2-carboxamide	IC50	0.51 nM	US-8969336: Diamino heterocyclic carboxamide compound
6-ethyl-3-[3-fluoro-4-(4-methylpiperazin-1-yl)anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide	IC50	0.58 nM	US-8969336: Diamino heterocyclic carboxamide compound
6-ethyl-5-[(4-hydroxycyclohexyl)amino]-3-[3-methyl-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]pyrazine-2-carboxamide	IC50	0.65 nM	US-8969336: Diamino heterocyclic carboxamide compound
1-[5-(1-hydroxy-2-methylpropan-2-yl)-1,2-oxazol-3-yl]-3-[4-[6-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl]urea	KD	0.68 nM	US-8551963: Imidazolothiazole compounds and methods of use thereof
US20250360145, Example 119	IC50	0.73 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
6-ethyl-5-[(4-hydroxy-4-methylcyclohexyl)amino]-3-[3-methyl-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]pyrazine-2-carboxamide	IC50	0.78 nM	US-8969336: Diamino heterocyclic carboxamide compound
US20250360145, Example 87	IC50	0.83 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
6-ethyl-5-[(4-hydroxycyclohexyl)amino]-3-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]pyrazine-2-carboxamide	IC50	0.86 nM	US-8969336: Diamino heterocyclic carboxamide compound
6-ethyl-5-[(4-hydroxy-4-methylcyclohexyl)amino]-3-[3-methyl-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]pyrazine-2-carboxamide	IC50	0.86 nM	US-8969336: Diamino heterocyclic carboxamide compound
4-[[5-[5-(7-azabicyclo[2.2.1]heptan-7-ylmethyl)-2-pyridinyl]-2-(butylamino)pyrimidin-4-yl]amino]cyclohexan-1-ol	IC50	0.86 nM	US-9649309: Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
6-ethyl-5-[(4-hydroxycyclohexyl)amino]-3-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]-3-(trifluoromethyl)anilino]pyrazine-2-carboxamide	IC50	1 nM	US-8969336: Diamino heterocyclic carboxamide compound
4-[[5-[5-[(1-adamantylamino)methyl]-2-pyridinyl]-2-(butylamino)pyrimidin-4-yl]amino]cyclohexan-1-ol	IC50	1 nM	US-9649309: Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
6-ethyl-3-[3-methyl-4-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide	IC50	1.2 nM	US-8969336: Diamino heterocyclic carboxamide compound
N-[3-[2-[4-(4-methylpiperazin-1-yl)anilino]-7-oxopteridin-8-yl]phenyl]prop-2-enamide	IC50	1.2 nM	US-9670213: Pteridine ketone derivative and applications thereof as EGFR, BLK, and FLT3 inhibitor
1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-[10-[2-[(1S,4S)-2,5-diazabicyclo[2.2.1]heptan-2-yl]ethoxy]-7-thia-2,5,9-triazatricyclo[6.4.0.02,6]dodeca-1(8),3,5,9,11-pentaen-4-yl]phenyl]urea	IC50	1.2 nM	US-9216997: Tri-heterocyclic derivatives, preparation process and uses thereof
4-[[2-(butylamino)-5-[5-[[(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)amino]methyl]-2-pyridinyl]pyrimidin-4-yl]amino]cyclohexan-1-ol	IC50	1.2 nM	US-9649309: Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
4-[[2-(4-methylanilino)-5-[5-(pyrrolidin-1-ylmethyl)-2-pyridinyl]pyrimidin-4-yl]amino]cyclohexan-1-ol	IC50	1.2 nM	US-9649309: Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
US20250360145, Example 83	IC50	1.2 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
6-ethyl-3-[3-methyl-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide	IC50	1.3 nM	US-8969336: Diamino heterocyclic carboxamide compound
4-[[2-(3-fluoroanilino)-5-[5-(pyrrolidin-1-ylmethyl)-2-pyridinyl]pyrimidin-4-yl]amino]cyclohexan-1-ol	IC50	1.3 nM	US-9649309: Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
4-[[2-(4-fluoroanilino)-5-[5-(pyrrolidin-1-ylmethyl)-2-pyridinyl]pyrimidin-4-yl]amino]cyclohexan-1-ol	IC50	1.5 nM	US-9649309: Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity
4-[2-(butylamino)-5-[4-(4-methylpiperazin-1-yl)phenyl]pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexan-1-ol	IC50	1.5 nM	US-10004755: Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity
1-[5-(1,3-dihydroxy-2-methylpropan-2-yl)-1,2-oxazol-3-yl]-3-[4-[6-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl]urea	KD	1.6 nM	US-8551963: Imidazolothiazole compounds and methods of use thereof
6-chloro-5-[(4-hydroxycyclohexyl)amino]-3-[3-methyl-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]pyrazine-2-carboxamide	IC50	1.6 nM	US-8969336: Diamino heterocyclic carboxamide compound
Staurosporine	KD	1.7 nM
6-ethyl-3-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide	IC50	1.9 nM	US-8969336: Diamino heterocyclic carboxamide compound
Gilteritinib	IC50	1.9 nM	US-8969336: Diamino heterocyclic carboxamide compound
(4R)-4-[(1R)-1-[[7-[3-methoxy-4-(trifluoromethoxy)phenyl]-1,6-naphthyridin-5-yl]oxy]ethyl]pyrrolidin-2-one	IC50	1.9 nM	US-8969568: Substituted naphthyridines and their use as medicaments
FORETINIB	IC50	1.9 nM
US20250360145, Example 101	IC50	1.9 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
4-[5-[4-(azepan-4-ylamino)phenyl]-2-(butylamino)pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexan-1-ol	IC50	2 nM	US-10004755: Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity
8-(4-methylcyclohexyl)-N-(5,6,7,8-tetrahydro-1,6-naphthyridin-2-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine	IC50	2.1 nM	US-8623885: Fused tricyclic dual inhibitors of CDK 4/6 and FLT3
4-[2-(4-hydroxybutylamino)-5-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexan-1-ol	IC50	2.1 nM	US-10004755: Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity
3-methoxy-8-[[5-methoxy-6-[(5-methoxy-2-pyridinyl)methoxy]-3-pyridinyl]methyl]-1,5-naphthyridine	IC50	2.1 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
US20250360145, Example 93	IC50	2.1 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
US20250360145, Example 56	IC50	2.2 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
US20250360145, Example 72	IC50	2.2 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
US20250360145, Example 100	IC50	2.2 nM	US-20250360145: CSF-1R INHIBITORS AND USES THEREOF
N-[3-[2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-7-oxopteridin-8-yl]phenyl]prop-2-enamide	IC50	2.36 nM	US-9670213: Pteridine ketone derivative and applications thereof as EGFR, BLK, and FLT3 inhibitor
2-hydroxy-1-[2-[[8-(4-methylcyclohexyl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-yl]amino]-7,8-dihydro-5H-1,6-naphthyridin-6-yl]ethanone	IC50	2.4 nM	US-8623885: Fused tricyclic dual inhibitors of CDK 4/6 and FLT3
8-(4-methylcyclohexyl)-N-[6-(2-methylsulfonylethyl)-7,8-dihydro-5H-1,6-naphthyridin-2-yl]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine	IC50	2.4 nM	US-8623885: Fused tricyclic dual inhibitors of CDK 4/6 and FLT3
4-[[2-(4-methoxyanilino)-5-[5-(pyrrolidin-1-ylmethyl)-2-pyridinyl]pyrimidin-4-yl]amino]cyclohexan-1-ol	IC50	2.4 nM	US-9649309: Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity

ChEMBL bioactivities

6100 potent at pChembl≥5 of 6100 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Kd	0.01	nM	CHEMBL5176837
11.00	Kd	0.01	nM	CHEMBL5927784
10.92	Kd	0.012	nM	CHEMBL5176837
10.82	IC50	0.015	nM	CHEMBL4744130
10.81	Kd	0.0154	nM	CHEMBL5195819
10.80	Kd	0.016	nM	CRENOLANIB
10.77	Kd	0.017	nM	CHEMBL6078253
10.68	Kd	0.021	nM	CHEMBL6002371
10.62	IC50	0.024	nM	CHEMBL5440655
10.60	Kd	0.025	nM	CHEMBL5927784
10.47	Kd	0.034	nM	CHEMBL6078253
10.42	IC50	0.038	nM	CHEMBL4519741
10.30	IC50	0.05	nM	CHEMBL6191359
10.30	IC50	0.05	nM	CHEMBL6191849
10.30	IC50	0.05	nM	CHEMBL6192901
10.30	IC50	0.05	nM	CHEMBL6189235
10.25	Kd	0.056	nM	CHEMBL6078253
10.22	IC50	0.06	nM	CRENOLANIB
10.22	IC50	0.06	nM	CHEMBL6192930
10.21	IC50	0.061	nM	CHEMBL5641913
10.21	IC50	0.061	nM	CHEMBL5641673
10.20	IC50	0.063	nM	CHEMBL5639694
10.20	IC50	0.063	nM	CHEMBL5639591
10.19	Kd	0.065	nM	CHEMBL6002371
10.14	IC50	0.072	nM	CHEMBL4790915
10.13	Kd	0.074	nM	CHEMBL6078253
10.10	IC50	0.08	nM	CHEMBL6188781
10.10	IC50	0.08	nM	CHEMBL6189029
10.10	IC50	0.08	nM	CHEMBL6192679
10.05	IC50	0.09	nM	CHEMBL6191366
10.03	Kd	0.093	nM	CHEMBL256961
10.00	IC50	0.101	nM	CHEMBL4086149
10.00	IC50	0.1	nM	CHEMBL4513768
10.00	Ki	0.1	nM	CHEMBL4864449
10.00	Ki	0.1	nM	CHEMBL4870188
10.00	IC50	0.1	nM	CHEMBL5268237
10.00	Kd	0.1	nM	CHEMBL6078253
10.00	Ki	0.1	nM	CHEMBL273187
9.99	IC50	0.102	nM	CHEMBL5639373
9.96	IC50	0.11	nM	CHEMBL5593388
9.96	Kd	0.11	nM	CHEMBL6002371
9.93	IC50	0.118	nM	CHEMBL5647067
9.93	IC50	0.117	nM	CHEMBL5646935
9.92	IC50	0.121	nM	CHEMBL5440655
9.92	IC50	0.119	nM	CHEMBL5646820
9.92	Kd	0.12	nM	CHEMBL6002371
9.91	IC50	0.123	nM	CHEMBL3612622
9.89	IC50	0.13	nM	CHEMBL4092761
9.88	IC50	0.132	nM	CHEMBL5639601
9.85	IC50	0.14	nM	CHEMBL6190161

PubChem BioAssay actives

2949 with measured affinity, of 6100 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
6-[7-methoxy-6-(1-methylpyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]-N-pyrrolidin-3-ylpyridin-2-amine	1894563: Binding affinity to FLT3-ITD-D835V mutant (unknown origin) assessed as dissociation constant	kd	<0.0001	uM
1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[3-fluoro-4-(1H-imidazo[4,5-b]pyridin-7-yloxy)phenyl]urea	1696916: Inhibition of FLT3 ITD mutant (unknown origin) expressed in mouse BaF3 cells	ic50	<0.0001	uM
2-[(E)-[2-(2-hydroxy-1H-indol-3-yl)indol-3-ylidene]amino]oxy-1-piperazin-1-ylethanone;hydrochloride	1868178: Binding affinity to FLT3 ITD/F691L double mutant (unknown origin) by KINOMEscan assay	kd	<0.0001	uM
N-[(5-methyl-1H-imidazol-2-yl)methyl]-4-(8,9,10,11-tetrahydro-3H-pyrazolo[4,5-a]phenanthridin-7-yl)benzamide	2003941: Inhibition of FLT3 D835Y mutant (unknown origin)	ic50	<0.0001	uM
Ponatinib	2183012: Inhibition of FLT3-ITD F691I mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hrs by CellTiter 96 aqueous one solution assay	ic50	<0.0001	uM
1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine	1562814: Inhibition of FLT3 D835Y mutant (unknown origin)	ic50	0.0001	uM
5-chloro-3-[1-(2-methyl-5-nitrophenyl)sulfonylpyrrol-3-yl]pyrazolo[1,5-a]pyrimidine	1245695: Inhibition of FLT3 (unknown origin) using biotin-Glu-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 as substrate after 90 mins by luminescence assay	ic50	0.0001	uM
1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]urea	1696916: Inhibition of FLT3 ITD mutant (unknown origin) expressed in mouse BaF3 cells	ic50	0.0001	uM
N-[6-(4-ethylpiperazin-1-yl)-2-methylpyrimidin-4-yl]-5-pyridin-4-yl-1,3-thiazol-2-amine;hydrochloride	1581288: Inhibition of wild type FLT3 (unknown origin) expressed in HEK293T cells assessed as decrease in FLT3 phosphorylation at 0.1 to 1000 nM after 1 hr by Western blot analysis	ic50	0.0001	uM
4-[(6-ethylthieno[2,3-d]pyrimidin-4-yl)amino]-N-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1H-pyrazole-5-carboxamide	1489804: Inhibition of human FLT3 using EAIYAAPFAKKK as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition measure after 120 mins by filter binding method	ic50	0.0001	uM
N-[4-(diethylaminomethyl)phenyl]-4-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide	1489804: Inhibition of human FLT3 using EAIYAAPFAKKK as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition measure after 120 mins by filter binding method	ic50	0.0001	uM
N-[(2S,4S,6R)-2,6-dimethyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-N-methylbenzamide	1691299: Inhibition of human FLT3 D835Y mutant EAIYAAPFAKKK peptide as substrate in presence of 33P-gamma ATP by hotspot kinase assay	ic50	0.0001	uM
1-[4-[3-[[4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-yl]amino]phenyl]-1,4-diazepan-1-yl]ethanone	1756404: Inhibition of FLT3 ITD mutant (unknown origin) using Glu/Tyr peptide substrate incubated for 120 mins measured after 40 mins incubation under dark by ADP-glo based luminescence assay	ki	0.0001	uM
1-[4-[4-[[4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-yl]amino]phenyl]piperazin-1-yl]ethanone	1756404: Inhibition of FLT3 ITD mutant (unknown origin) using Glu/Tyr peptide substrate incubated for 120 mins measured after 40 mins incubation under dark by ADP-glo based luminescence assay	ki	0.0001	uM
3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-N-[(3R)-pyrrolidin-3-yl]-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
(4-aminopiperidin-1-yl)-[3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-indazol-5-yl]methanone	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
N-(3-aminopropyl)-3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
N-[(1S,3S)-3-aminocyclopentyl]-3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
N-(3-aminopropyl)-3-(6-piperidin-1-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
N-[(1S,3R)-3-aminocyclopentyl]-3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
N-[(1S,3S)-3-aminocyclopentyl]-3-(6-methoxy-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143349: Inhibition of recombinant FLT3 D835Y mutant (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-N-[[(3S)-pyrrolidin-3-yl]methyl]-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
N-[3-(dimethylamino)propyl]-3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-N-[[(3R)-pyrrolidin-3-yl]methyl]-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
N-(4-aminocyclohexyl)-3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0001	uM
(15S,16R,18R)-16-amino-N,15-dimethyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxamide	1927343: Inhibition of FLT3 (unknown origin) autophosphorylation expressed in human Leukemia cells	ic50	0.0001	uM
3-N-[4-(4-morpholin-4-ylcyclohexyl)phenyl]-1-pyridin-2-yl-1,2,4-triazole-3,5-diamine	649408: Inhibition of human recombinant FLT3 by radiometric assay	ki	0.0002	uM
N-[(E)-(5-cyanopyrazolo[1,5-a]pyrimidin-3-yl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide	1245695: Inhibition of FLT3 (unknown origin) using biotin-Glu-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 as substrate after 90 mins by luminescence assay	ic50	0.0002	uM
N-[2-(5-chloropyrazolo[1,5-a]pyrimidin-3-yl)ethyl]-2-methyl-5-nitrobenzenesulfonamide	1245695: Inhibition of FLT3 (unknown origin) using biotin-Glu-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 as substrate after 90 mins by luminescence assay	ic50	0.0002	uM
N-[2-(5-chloropyrazolo[1,5-a]pyrimidin-3-yl)ethyl]-5-cyano-N,2-dimethylbenzenesulfonamide	1245695: Inhibition of FLT3 (unknown origin) using biotin-Glu-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 as substrate after 90 mins by luminescence assay	ic50	0.0002	uM
4-[(2-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)amino]-N-(4-piperazin-1-ylphenyl)-1H-pyrazole-5-carboxamide	1360758: Inhibition of human FLT3 by Hotspot assay	ic50	0.0002	uM
2-[4-(4-acetylpiperazin-1-yl)anilino]-4-(1H-indazol-3-yl)pyrimidine-5-carbonitrile	1756404: Inhibition of FLT3 ITD mutant (unknown origin) using Glu/Tyr peptide substrate incubated for 120 mins measured after 40 mins incubation under dark by ADP-glo based luminescence assay	ki	0.0002	uM
2-[(E)-[2-(2-hydroxy-1H-indol-3-yl)indol-3-ylidene]amino]oxy-N-[(3S)-pyrrolidin-3-yl]acetamide;hydrochloride	1868174: Inhibition of human recombinant His-tagged FLT3/D835Y mutant expressed in baculovirus expression system incubated for 30 mins in presence of ATP by HTRF analysis	ic50	0.0002	uM
2-[(E)-[2-(5-chloro-2-hydroxy-1H-indol-3-yl)indol-3-ylidene]amino]oxy-1-piperazin-1-ylethanone;hydrochloride	1868174: Inhibition of human recombinant His-tagged FLT3/D835Y mutant expressed in baculovirus expression system incubated for 30 mins in presence of ATP by HTRF analysis	ic50	0.0002	uM
2-[(E)-[2-(2-hydroxy-1H-indol-3-yl)indol-3-ylidene]amino]oxy-N-[(3R)-pyrrolidin-3-yl]acetamide;hydrochloride	1868174: Inhibition of human recombinant His-tagged FLT3/D835Y mutant expressed in baculovirus expression system incubated for 30 mins in presence of ATP by HTRF analysis	ic50	0.0002	uM
2-[(E)-[2-(5-fluoro-2-hydroxy-1H-indol-3-yl)indol-3-ylidene]amino]oxy-1-piperazin-1-ylethanone;hydrochloride	1868174: Inhibition of human recombinant His-tagged FLT3/D835Y mutant expressed in baculovirus expression system incubated for 30 mins in presence of ATP by HTRF analysis	ic50	0.0002	uM
2-[(E)-[2-(5-bromo-2-hydroxy-1H-indol-3-yl)indol-3-ylidene]amino]oxy-1-piperazin-1-ylethanone;hydrochloride	1868174: Inhibition of human recombinant His-tagged FLT3/D835Y mutant expressed in baculovirus expression system incubated for 30 mins in presence of ATP by HTRF analysis	ic50	0.0002	uM
N-[(1S,3S)-3-aminocyclopentyl]-3-[6-(furan-3-yl)-1H-benzimidazol-2-yl]-1H-indazole-5-carboxamide	2143349: Inhibition of recombinant FLT3 D835Y mutant (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0002	uM
3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-N-(piperidin-3-ylmethyl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0002	uM
N-(3-aminopropyl)-3-(6-pyrrolidin-1-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0002	uM
N-(3-amino-2-methylpropyl)-3-(6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143345: Inhibition of recombinant wild type FLT3 kinase domain (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0002	uM
N-[(1S,3S)-3-aminocyclopentyl]-3-(6-pyrrolidin-1-yl-1H-benzimidazol-2-yl)-1H-indazole-5-carboxamide	2143349: Inhibition of recombinant FLT3 D835Y mutant (unknown origin) using peptide substrate incubated for for 30 mins by HTRF assay	ic50	0.0002	uM
3,3,3-trifluoro-1-[4-[[2-[[6-(2-methyl-4-pyridinyl)-1H-benzimidazol-2-yl]amino]-4-pyridinyl]methyl]piperazin-1-yl]propan-1-one	1582167: Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues) expressed in sf21 cells using biotin labelled Ahx-GGEEEEYFELVKKKK peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubated for 45 mins in presence of 10 uM of ATP by TR-FRET assay	ic50	0.0003	uM
1-[[6-[4-[2-(2-hydroxyethylamino)ethoxy]phenyl]-5-methyl-2-thiophen-2-ylthieno[2,3-d]pyrimidin-4-yl]amino]-3-methylpyrrole-2,5-dione;hydrochloride	1317473: Inhibition of human FLT3 D835Y mutant preincubated for 15 mins followed by poly(Glu:Tyr) substrate addition for 30 mins in presence of [gamma-32P]ATP by TR-FRET assay	ic50	0.0003	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	1425006: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0003	uM
5-fluoro-3-[(3E)-3-(2-piperazin-1-ylethoxyimino)indol-2-yl]-1H-indol-2-ol	1868174: Inhibition of human recombinant His-tagged FLT3/D835Y mutant expressed in baculovirus expression system incubated for 30 mins in presence of ATP by HTRF analysis	ic50	0.0003	uM
N-[4-(piperazin-1-ylmethyl)phenyl]-4-(thieno[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide	1489804: Inhibition of human FLT3 using EAIYAAPFAKKK as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition measure after 120 mins by filter binding method	ic50	0.0003	uM
N-[4-[(4-methyl-1,4-diazepan-1-yl)methyl]phenyl]-4-(thieno[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide	1489804: Inhibition of human FLT3 using EAIYAAPFAKKK as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition measure after 120 mins by filter binding method	ic50	0.0003	uM
8-(4-aminophenyl)-2-[3-methyl-4-(4-methylpiperazin-1-yl)anilino]pteridin-7-one	1635671: Binding affinity to human partial length FLT3 D835V mutant (592 to 969 residues) expressed in mammalian expression system after 1 hr	kd	0.0003	uM
N-(2,4-dimethoxyphenyl)-4-(1H-indol-3-yl)pyrimidin-2-amine	1927363: Binding affinity to human FLT3 assessed as inhibition constant	ki	0.0003	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Sorafenib	increases response to substance, decreases reaction, increases phosphorylation, decreases activity, decreases phosphorylation	5
ponatinib	decreases activity, decreases reaction, increases phosphorylation, decreases phosphorylation	4
Arsenic Trioxide	decreases reaction, increases expression, affects binding, increases reaction, decreases phosphorylation (+1 more)	3
Benzo(a)pyrene	affects methylation, decreases expression, increases methylation	3
sodium arsenite	increases expression, increases phosphorylation	2
Semaxinib	decreases activity	2
Tretinoin	affects cotreatment, decreases expression, increases reaction, increases response to substance	2
2-hydroxy-1-(2-((9-(4-methylcyclohexyl)-9H-pyrido(4’,3’-4,5)pyrrolo(2,3-d)pyrimidin-2-yl)amino)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl)ethanone	decreases phosphorylation	1
pexidartinib	decreases activity	1
RGFP966	affects reaction, decreases expression, decreases phosphorylation	1
bisphenol F	affects cotreatment, increases methylation	1
S63845	decreases expression, increases reaction	1
parthenolide	increases reaction, decreases expression	1
fulvic acid	affects cotreatment, decreases reaction, increases expression	1
bisphenol A	increases expression	1
ethyl-p-hydroxybenzoate	decreases expression	1
terbufos	increases methylation	1
benzo(e)pyrene	increases methylation	1
celastrol	decreases expression	1
bafilomycin A	increases degradation, decreases reaction, increases expression	1
midostaurin	decreases response to substance, decreases activity	1
romidepsin	decreases phosphorylation, increases reaction	1
gedunin	decreases expression	1
tanespimycin	decreases expression	1
SU 5614	decreases activity	1
D-65476	increases reaction, affects cotreatment, decreases expression	1
THRX 165724	decreases phosphorylation	1
NSC 23766	affects response to substance	1
palbociclib	affects response to substance, decreases expression, decreases phosphorylation	1
5-((5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl)-N-(2-hydroxy-3-morpholin-4-ylpropyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide	decreases phosphorylation	1

ChEMBL screening assays

3132 unique, capped per target: 3096 binding, 24 functional, 8 admet, 4 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1003890	Binding	Inhibition of Flt3	Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities. — J Med Chem
CHEMBL1963779	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: FLT3	PubChem BioAssay data set
CHEMBL3826089	ADMET	Inhibition of FLT3 (unknown origin)	Discovery of a potent and highly selective transforming growth factor β receptor-associated kinase 1 (TAK1) inhibitor by structure based drug design (SBDD). — Bioorg Med Chem

Cellosaurus cell lines

189 cell lines: 144 cancer cell line, 39 factor-dependent cell line, 4 embryonic stem cell, 2 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_0064	MV4-11	Cancer cell line	Male
CVCL_0138	ACH-2	Cancer cell line	Female
CVCL_0207	CCRF-CEM	Cancer cell line	Female
CVCL_0614	Kasumi-6	Cancer cell line	Male
CVCL_0R18	CEM-TART clone 1A2	Cancer cell line	Female
CVCL_0U11	CEM/MX1	Cancer cell line	Female
CVCL_1150	CTV-1	Cancer cell line	Male
CVCL_1B35	CEM/VM-1	Cancer cell line	Female
CVCL_1E04	Rev-CEM	Cancer cell line	Female
CVCL_1G53	CEM-GFP	Cancer cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00199147	PHASE4	UNKNOWN	Efficacy of G-CSF-Priming in Elderly AML Patients
NCT00304447	PHASE4	COMPLETED	Study Evaluating the Effect of Corticosteroids on Mylotarg® Infusion-Related Adverse Events in Patients With Leukemia
NCT00464217	PHASE4	COMPLETED	Treatment of the Acute Myeloblastic Leukaemia in Patients Over 65 Years
NCT00487448	PHASE4	COMPLETED	SMD_FLAG-IDA_98: FLAG-IDA in Induction Treatment of High Risk Myelodysplastic Syndromes or Secondary Acute Myeloblastic Leukemia
NCT00488709	PHASE4	COMPLETED	Fludarabine, Cytarabine, Topotecan in Treating Patients With Relapsed or Refractory Acute Myeloid Leukemia
NCT00686543	PHASE4	COMPLETED	Oral Posaconazole in High Risk Patients With Gastrointestinal Dysfunction (Study P05115)
NCT01041040	PHASE4	COMPLETED	LAM07: Study to Analyze the Efficacy of a Risk Adapted Treatment Strategy, Including Gemtuzumab Ozogamicin (GO) During Consolidation, for Patients With Acute Myeloid Leukemia (AML)
NCT01198054	PHASE4	TERMINATED	LENA-LMA-5:Lenalidomide in Acute Myeloid Leukemia (AML)
NCT01200355	PHASE4	COMPLETED	Posaconazole Versus Micafungin for Prophylaxis Against Invasive Fungal Infections During Neutropenia in Patients Undergoing Chemotherapy for Acute Myelogenous Leukemia, Acute Lymphocytic Leukemia or Myelodysplastic Syndrome
NCT01347996	PHASE4	COMPLETED	Maintenance Therapy With Ceplene® (Histamine) and IL-2 on Immune Response and MRD in Acute Myeloid Leukemia
NCT01587430	PHASE4	UNKNOWN	3 Anthracyclines, 2 Types of Consolidation With Different ARA-C Doses and Maintenance in Adult Acute Myeloid Leukemia
NCT01819792	PHASE4	COMPLETED	Respiratory Viral Infections During Acute Myeloid Leukemia (AML)Chemotherapy Related Aplasia
NCT02024308	PHASE4	UNKNOWN	AML1-ETO Acute Myeloid Leukemia With Fludarabine and Cytarabine Chemotherapy
NCT02027064	PHASE4	UNKNOWN	Interferon for the Intervention of Molecular Relapse in t (8; 21) AML After Allo-HSCT
NCT02277847	PHASE4	UNKNOWN	Idarubicin at Different Dosages as Induction Therapy for Newly Diagnosed Acute Myeloid Leukaemia
NCT02386800	PHASE4	ACTIVE_NOT_RECRUITING	CINC424A2X01B Rollover Protocol
NCT02926586	PHASE4	COMPLETED	Fludarabine and Cytarabine Versus High-dose Cytarabine for CBF-AML
NCT02933333	PHASE4	UNKNOWN	G-CSF Alone or Combination With GM-CSF on Prevention and Treatment of Infection in Children With Malignant Tumor
NCT03026842	PHASE4	UNKNOWN	Decitabine Versus Conventional Chemotherapy for Maintenance Therapy of Acute Myeloid Leukemia With t(8;21)
NCT03150134	PHASE4	UNKNOWN	Early Tapering of Immunosuppressive Agents to Immunomodulation to Improve Survival of AML Patients
NCT05144243	PHASE4	ACTIVE_NOT_RECRUITING	Study to Assess Adverse Events and Change in Disease State of Oral Venetoclax in Combination With Subcutaneous (SC) Azacitidine in Newly Diagnosed Adult Participants With Acute Myeloid Leukemia (AML) Who Are Ineligible for Intensive Chemotherapy in China
NCT06370000	PHASE4	RECRUITING	Oral Azacitidine in Transplant-Eligible Patients With Acute Myeloid Leukemia (AML) Suffering From Health-Inequality
NCT06571825	PHASE4	RECRUITING	RIC Allo-HSCT vs. Venetoclax-Based Consolidation in Elderly AML Patients After First CR
NCT07016165	PHASE4	RECRUITING	Ciprofloxacin vs Ceftazidime for Empirical Treatment of High-Risk Neutropenic Fever in Children With Hematologic Malignancies
NCT07044687	PHASE4	RECRUITING	Study to Assess Adverse Events and Change in Disease Activity of Oral Venetoclax in Combination With Subcutaneous (SC) or Intravenous (IV) Azacitidine in Newly Diagnosed Adult Participants With Acute Myeloid Leukemia (AML) Who Are Ineligible for Standard Induction Therapy in India
NCT07486713	PHASE4	RECRUITING	Olutasidenib DDI Study in Patients With IDH1 Mutation Positive Malignancies
NCT07561892	PHASE4	RECRUITING	Study of the Effectiveness and Safety of Daunorubicin /Idarubicin ± Silibinin in Treating Newly Diagnosed AML (Non-M3).
NCT00000589	PHASE3	COMPLETED	Trial to Reduce Alloimmunization to Platelets (TRAP)
NCT00044486	PHASE3	COMPLETED	Prophylaxis Trial of Posaconazole Versus Standard Azole Therapy for Neutropenic Patients (Study P01899)
NCT00093990	PHASE3	COMPLETED	Tipifarnib Versus Best Supportive Care in the Treatment of Newly Diagnosed Acute Myeloid Leukemia (AML)
NCT00125606	PHASE3	TERMINATED	Phase 3 Trial for AML Patients in CR2 Comparing 8Gy TBI /Fludarabine to Conditioning With TBI 12Gy/Cyclophosphamide
NCT00136084	PHASE3	COMPLETED	Treatment of Patients With Newly Diagnosed Acute Myeloid Leukemia or Myelodysplasia
NCT00146120	PHASE3	COMPLETED	Risk-Adapted Therapy of Acute Myeloid Leukemia of Adults (18-60 Years) According to the Cytogenetic Result
NCT00150878	PHASE3	TERMINATED	Standard vs. Reduced-Intensity Conditioning in Patients With Acute Myeloid Leukemia in First Remission
NCT00151255	PHASE3	COMPLETED	All-Trans Retinoic Acid in Combination With Standard Induction and Consolidation Therapy in Older Patients With Newly Diagnosed Acute Myeloid Leukemia
NCT00152139	PHASE3	COMPLETED	Stem Cell Transplantation for Patients With Hematologic Malignancies
NCT00152594	PHASE3	TERMINATED	Voriconazole or Placebo in the Prophylaxis of Lung Infiltrates in Patients Undergoing Induction Chemotherapy for Acute Myelogenous Leukemia
NCT00186966	PHASE3	COMPLETED	Treatment of Children and Adolescents With Refractory or Relapsed Acute Myeloid Leukemia
NCT00226512	PHASE3	WITHDRAWN	To Determine the Role of Adding Campath-1H or ATG Given In-vivo in Addition to Fludarabine and Low Dose Busulfex on Outcome in Patients Treated With Reduced Intensity Conditioning
NCT00260832	PHASE3	COMPLETED	Trial of Decitabine in Patients With Acute Myeloid Leukemia