MLLT3

Summary

MLLT3 (MLLT3 super elongation complex subunit, HGNC:7136) is a protein-coding gene on chromosome 9p21.3, encoding Protein AF-9 (P42568). Chromatin reader component of the super elongation complex (SEC), a complex required to increase the catalytic rate of RNA polymerase II transcription by suppressing transient pausing by the polymerase at multiple sites along the DNA.

Enables chromatin binding activity; lysine-acetylated histone binding activity; and molecular adaptor activity. Involved in several processes, including hematopoietic stem cell differentiation; positive regulation of DNA-templated transcription; and regulation of stem cell division. Acts upstream of or within negative regulation of canonical Wnt signaling pathway and positive regulation of Wnt signaling pathway, planar cell polarity pathway. Located in cytosol and nucleoplasm. Part of transcription elongation factor complex.

Source: NCBI Gene 4300 — RefSeq curated summary.

At a glance

• GWAS associations: 11
• Clinical variants (ClinVar): 88 total
• Druggable target: yes
• Cancer driver (intOGen): ambiguous (mixed evidence) across 1 cancer types
• MANE Select transcript: NM_004529

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:7136
Approved symbol	MLLT3
Name	MLLT3 super elongation complex subunit
Location	9p21.3
Locus type	gene with protein product
Status	Approved
Aliases	AF-9, AF9, YEATS3
Ensembl gene	ENSG00000171843
Ensembl biotype	protein_coding
OMIM	159558
Entrez	4300

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 6 protein_coding, 2 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000380321, ENST00000380338, ENST00000468513, ENST00000469261, ENST00000475957, ENST00000488705, ENST00000491137, ENST00000629733, ENST00000630269

RefSeq mRNA: 2 — MANE Select: NM_004529 NM_001286691, NM_004529

CCDS: CCDS6494, CCDS69579

Canonical transcript exons

ENST00000380338 — 11 exons

Exon	Start	End
ENSE00001280089	20341669	20346574
ENSE00001620972	20622245	20622499
ENSE00003482069	20365669	20365744
ENSE00003572058	20360742	20360841
ENSE00003592056	20353525	20353596
ENSE00003609015	20413721	20414425
ENSE00003616346	20363476	20363605
ENSE00003628570	20456704	20456786
ENSE00003665608	20620654	20620834
ENSE00003670233	20448123	20448266
ENSE00003671120	20354808	20354879

Expression profiles

Bgee: expression breadth ubiquitous, 251 present calls, max score 98.91.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 16.5015 / max 444.7036, expressed in 1632 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
100198	9.0587	1552
100197	3.4232	1045
100196	1.8947	601
100186	1.3779	105
100195	0.4789	198
100194	0.2680	80

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
ganglionic eminence	UBERON:0004023	98.91	gold quality
cortical plate	UBERON:0005343	97.78	gold quality
embryo	UBERON:0000922	95.17	gold quality
rectum	UBERON:0001052	93.64	gold quality
calcaneal tendon	UBERON:0003701	90.94	gold quality
colonic epithelium	UBERON:0000397	90.59	gold quality
endothelial cell	CL:0000115	89.81	gold quality
ventricular zone	UBERON:0003053	89.68	gold quality
buccal mucosa cell	CL:0002336	89.63	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	88.35	gold quality
mucosa of transverse colon	UBERON:0004991	87.25	gold quality
stromal cell of endometrium	CL:0002255	87.24	gold quality
islet of Langerhans	UBERON:0000006	86.57	gold quality
sural nerve	UBERON:0015488	85.90	gold quality
transverse colon	UBERON:0001157	85.73	gold quality
right lobe of thyroid gland	UBERON:0001119	85.72	gold quality
left lobe of thyroid gland	UBERON:0001120	85.68	gold quality
thyroid gland	UBERON:0002046	85.68	gold quality
gall bladder	UBERON:0002110	85.35	gold quality
colon	UBERON:0001155	84.66	gold quality
large intestine	UBERON:0000059	84.58	gold quality
muscle layer of sigmoid colon	UBERON:0035805	84.53	gold quality
periodontal ligament	UBERON:0008266	84.23	gold quality
right adrenal gland cortex	UBERON:0035827	84.21	gold quality
sigmoid colon	UBERON:0001159	84.11	gold quality
primary visual cortex	UBERON:0002436	83.64	gold quality
right adrenal gland	UBERON:0001233	83.57	gold quality
intestine	UBERON:0000160	83.51	gold quality
left adrenal gland	UBERON:0001234	83.47	gold quality
minor salivary gland	UBERON:0001830	83.17	gold quality

Single-cell (SCXA)

Detected in 10 experiment(s), a significant marker in 7.

Experiment	Marker?	Max mean expression
E-CURD-6	yes	687.28
E-MTAB-9067	yes	617.93
E-HCAD-6	yes	32.76
E-CURD-119	yes	30.95
E-ANND-3	yes	12.25
E-CURD-112	yes	6.79
E-GEOD-83139	yes	4.29
E-MTAB-7249	no	2148.11
E-GEOD-100618	no	1261.53
E-GEOD-86618	no	206.16

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

4 targets.

Target	Regulation
BAX	Repression
CDKN1A	Repression
MDM2	Repression
SCNN1A	Activation

Upstream regulators (CollecTRI, top): NR3C2

miRNA regulators (miRDB)

218 targeting MLLT3, 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-5011-5P	100.00	83.46	5820
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-511-3P	99.99	68.85	1467
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-4650-5P	99.98	64.69	999
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753
HSA-MIR-548T-3P	99.96	70.64	3753
HSA-MIR-1250-3P	99.96	70.04	4038

Literature-anchored findings (GeneRIF, showing 40)

• In the Acute Myeloid Leukemia patients, detected MLL rearrangements consisting of MLL/AF6, MLL/AF9, MLL/AF17 , MLL/ELL and MLL partial tandem duplication. MLL rearrangement include chromosome translocation and partial tandem duplication. (PMID:16086288)
• The patients with immunophenotype of Pre-B-acute lymphoblastic leukemia were found to carry: MLL/AF9. (PMID:16215946)
• Down-regulation of AF9 is not necessary to abolish malignant phenotypes by induction of terminal monocyte-macrophage differentiation in leukaemic cells carrying t(9;11)(p22;q23). (PMID:16328057)
• demonstrate coimmunoprecipitation of the All1/Af4 and All1/Af9 fusions with Drosha, disrupted by treatment with DNase I (PMID:17581865)
• MLLT3 as a regulator of early erythroid and megakaryocytic cell fate in the human system. (PMID:18371451)
• Expression of MLL-AF9 in human CD34+ cells induces acute myeloid, lymphoid, or mixed-lineage leukemia in immunodeficient mice. (PMID:18538732)
• Diversin, containing several nuclear localization signals, translocates to the nucleus, where it interacts with the transcription factor AF9. (PMID:19591803)
• AF17 competes with AF9 to bind Dot1a, decreases Dot1a nuclear expression by possibly facilitating its nuclear export, and relieves Dot1a.AF9-mediated repression of alpha-ENaC and other target genes. (PMID:19864429)
• Ras activation seems to complement the MLLT3-MLL oncogene in transformation. (PMID:20395514)
• our data suggest: (i) C14ORF28, GNB2L1, MLLT3, DRD2 and DARPP-32 are important in the pathogenesis of schizophrenia and bipolar disorder (PMID:20874815)
• Within the group of MLL-AF9-positive patients, high BRE expression predicted superior survival, while normal BRE expression predicted extremely poor survival. (PMID:21937695)
• MLL-AF9-negative U937 cells but not positive MLL-AF9 THP-1 cells, suggesting that the toxocity ting was not antibody-mediated by antibodies against MLL-AF9 protein. (PMID:21959947)
• we identified a novel fusion gene consisted of PAX5 and MLLT3 during progression from chronic phase to blastic phase in chronic myeloid leukemia (PMID:22309891)
• Identification of genes that define transcription factor networks and important genetic pathways acting during progression of leukemia induced by MLL fusion oncogenes. (PMID:22427200)
• neonatal cells expressing MLL-AF9 were enriched for gene signatures associated with poor prognosis (PMID:23178754)
• AF9 functions as a signaling hub that regulates transcription through dynamic recruitment of cofactors in normal hematopoiesis and in acute leukemia. (PMID:23260655)
• We demonstrate that leukemogenic activity of MLL-AF9 requires RUVBL2 (RuvB-like 2), an AAA+ ATPase family member that functions in a wide range of cellular processes, including chromatin remodeling and transcriptional regulation. (PMID:23403462)
• Abrogation of Rac1 signaling causes DNA double-strand breaks in acute monocytic leukemia cells harbouring the MLL-AF9 oncogene. (PMID:23624644)
• Interaction with CBX8 precludes AF9-DOT1L binding. (PMID:23891621)
• Studies identified the evolutionarily conserved Af9 YEATS domain as a novel acetyllysine-binding module and established a direct link between histone acetylation and DOT1L-mediated H3K79 methylation in transcription control. (PMID:25417107)
• AF9 and its homolog ENL directly interact with AF4. (PMID:25509985)
• A luciferase reporter gene assay revealed that hsp70 promoter activation is enhanced by the transcriptional co-activator AF9 and splicing mediator SNRPE, but suppressed by the coiled-coil domain-containing protein CCDC127. (PMID:26873636)
• YEATS domain of AF9 directly links histone crotonylation to active transcription. (PMID:27105114)
• Exploring the mechanism how AF9 recognizes and binds H3K9ac by molecular dynamics simulations and free energy calculations. (PMID:27312527)
• Results show that human MLL-AF9 expression in mouse long-term hematopoietic stem cells causes invasive, chemoresistant acute myeloid leukemia that expresses genes related to epithelial-mesenchymal transition. (PMID:27344946)
• Results show that MLL-AF9 reduces Id2 and increases E2-2 expression to drive and sustain leukemia stem cell potential in MLL-rearranged acute myeloid leukemia (AML). Low expression of Id2 or of an Id2 gene signature is associated with poor prognosis in not only MLL-rearranged but also t(8;21) AML patients. (PMID:27374225)
• Structural insights into H3 histone crotonyl-lysine recognition by the AF9 YEATS domain have been presented. (PMID:27545619)
• MLL-AF9 fusion is associated with acute myeloid leukemia. (PMID:28114278)
• This system provides for rapid systematic screening of relative risk, dose dependence, and combinatorial impact of multitudes of dietary and environmental exposures on MLL-AF9 translocations (PMID:30387535)
• To study the ability of FLT3N676K to cooperate with KMT2A-MLLT3 in human leukemogenesis. (PMID:30953031)
• Characterization of Copy Number Variations in Oral Cavity Squamous Cell Carcinoma Reveals a Novel Role for MLLT3 in Cell Invasiveness. (PMID:31273053)
• MLLT3 thus acts as haematopoietic stem cells (HSCs) maintenance factor that links histone reader and modifying activities to modulate HSC gene expressio (PMID:31776511)
• Based on the observation that MLL-AF9 helps to preserve the ongoing gene expression program across multiple cellular contexts, study proposes that the rapidly proliferating, immature myeloid progenitor cell state initiates transformation when this cell state is perpetuated by MLL-AF9 expression, fulfilling the functional definition of malignancy. (PMID:31852898)
• BCOR Binding to MLL-AF9 Is Essential for Leukemia via Altered EYA1, SIX, and MYC Activity. (PMID:32954361)
• The miR-5694/AF9/Snail Axis Provides Metastatic Advantages and a Therapeutic Target in Basal-like Breast Cancer. (PMID:33221433)
• Relationships between AML1-ETO and MLL-AF9 fusion gene expressions and hematological parameters in acute myeloid leukemia. (PMID:33431365)
• The Transcriptional Coactivator, ALL1-Fused Gene From Chromosome 9, Simultaneously Sustains Hypoxia Tolerance and Metabolic Advantages in Liver Cancer. (PMID:33928666)
• The Intrinsically Disordered Proteins MLLT3 (AF9) and MLLT1 (ENL) - Multimodal Transcriptional Switches With Roles in Normal Hematopoiesis, MLL Fusion Leukemia, and Kidney Cancer. (PMID:34174329)
• The adverse impact of ecotropic viral integration site-1 (EVI1) overexpression on the prognosis of acute myeloid leukemia with KMT2A gene rearrangement in different risk stratification subtypes. (PMID:36358022)
• Molecular Recognition of Methacryllysine and Crotonyllysine by the AF9 YEATS Domain. (PMID:37108167)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	mllt3	ENSDARG00000006754
mus_musculus	Mllt3	ENSMUSG00000028496
rattus_norvegicus	Mllt3	ENSRNOG00000011280
drosophila_melanogaster	ear	FBGN0026441

Paralogs (2): MLLT1 (ENSG00000130382), YEATS2 (ENSG00000163872)

Protein

Protein identifiers

Protein AF-9 — P42568 (reviewed: P42568)

Alternative names: ALL1-fused gene from chromosome 9 protein, Myeloid/lymphoid or mixed-lineage leukemia translocated to chromosome 3 protein, YEATS domain-containing protein 3

All UniProt accessions (6): P42568, A0A0D9SF09, A0A0S2Z448, A0A6Q8PGU4, A0A6Q8PH64, B1APT5

UniProt curated annotations — full annotation on UniProt →

Function. Chromatin reader component of the super elongation complex (SEC), a complex required to increase the catalytic rate of RNA polymerase II transcription by suppressing transient pausing by the polymerase at multiple sites along the DNA. Specifically recognizes and binds acylated histone H3, with a preference for histone H3 that is crotonylated. Crotonylation marks active promoters and enhancers and confers resistance to transcriptional repressors. Recognizes and binds histone H3 crotonylated at ‘Lys-9’ (H3K9cr), and with slightly lower affinity histone H3 crotonylated at ‘Lys-18’ (H3K18cr). Also recognizes and binds histone H3 acetylated and butyrylated at ‘Lys-9’ (H3K9ac and H3K9bu, respectively), but with lower affinity than crotonylated histone H3. In the SEC complex, MLLT3 is required to recruit the complex to crotonylated histones. Recruitment of the SEC complex to crotonylated histones promotes recruitment of DOT1L on active chromatin to deposit histone H3 ‘Lys-79’ methylation (H3K79me). Plays a key role in hematopoietic stem cell (HSC) maintenance by preserving, rather than conferring, HSC stemness. Acts by binding to the transcription start site of active genes in HSCs and sustaining level of H3K79me2, probably by recruiting DOT1L. May play a role in leukemogenic gene transcription.

Subunit / interactions. Component of the super elongation complex (SEC), at least composed of EAF1, EAF2, CDK9, MLLT3/AF9, AFF (AFF1 or AFF4), the P-TEFb complex and ELL (ELL, ELL2 or ELL3). Interacts with BCOR. Interacts with CBX8. Interacts with ALKBH4. Interacts with acetylated or crotonylated KAT6A/MOZ; the interaction is direct.

Subcellular location. Nucleus. Chromosome.

Tissue specificity. Enriched in undifferentiated hematopoietic stem cells in fetal liver, cord blood and bone marrow.

Disease relevance. A chromosomal aberration involving MLLT3 is associated with acute leukemias. Translocation t(9;11)(p22;q23) with KMT2A/MLL1. The result is a rogue activator protein. Fusion protein KMT2A-MLLT3 interacts with MEN1 and PSIP1. A chromosomal aberration involving MLLT3 was observed in a patient with neuromotor development delay, cerebellar ataxia and epilepsy. Translocation t(4;9)(q35;p22).

Activity regulation. Crotonylated lysine binding is strongly inhibited by the peptide XL-07i, carrying a 2-furancarbonyl side chain and capped with a hydrophobic carboxybenzyl group. XL-07i targets the unique pi-pi-pi stacking interaction at the crotonylation recognition site.

Domain organisation. The YEATS domain specifically recognizes and binds acylated histones, with a marked preference for histones that are crotonylated. Also binds histone H3 acetylated at ‘Lys-9’ (H3K9ac), but with lower affinity. Binds crotonylated lysine through a non-canonical pi-pi-pi stacking mechanism. The YEATS domain also binds DNA.

Isoforms (2)

UniProt ID	Names	Canonical?
P42568-1	1	yes
P42568-2	2

RefSeq proteins (2): NP_001273620, NP_004520* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR038704	YEAST_sf	Homologous_superfamily
IPR040930	AF-9_AHD	Domain
IPR052790	YEATS_domain	Family
IPR055129	YEATS_dom	Domain

Pfam: PF03366, PF17793

UniProt features (57 total): mutagenesis site 11, strand 11, compositionally biased region 8, helix 6, modified residue 5, site 4, region of interest 3, sequence conflict 3, chain 1, domain 1, cross-link 1, splice variant 1, short sequence motif 1, turn 1

Structure

Experimental structures (PDB)

26 structures.

PDB	Method	Resolution (Å)
8PJ7	X-RAY DIFFRACTION	1.26
7VKG	X-RAY DIFFRACTION	1.83
5YYF	X-RAY DIFFRACTION	1.9
6MIL	X-RAY DIFFRACTION	1.93
7EIC	X-RAY DIFFRACTION	1.95
7EID	X-RAY DIFFRACTION	2
8TLX	X-RAY DIFFRACTION	2.1
9ARR	X-RAY DIFFRACTION	2.1
8TLW	X-RAY DIFFRACTION	2.11
6LS6	X-RAY DIFFRACTION	2.2
7VKH	X-RAY DIFFRACTION	2.25
4TMP	X-RAY DIFFRACTION	2.3
9ARO	X-RAY DIFFRACTION	2.3
6MIM	X-RAY DIFFRACTION	2.52
8TLV	X-RAY DIFFRACTION	2.66
5HJB	X-RAY DIFFRACTION	2.7
9IM4	X-RAY DIFFRACTION	2.79
5HJD	X-RAY DIFFRACTION	2.81
8Z73	X-RAY DIFFRACTION	2.91
6L5Z	X-RAY DIFFRACTION	3.05
2LM0	SOLUTION NMR
2MV7	SOLUTION NMR
2N4Q	SOLUTION NMR
2NDF	SOLUTION NMR
2NDG	SOLUTION NMR
6B7G	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P42568-F1	63.10	0.34

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 (4): 58 (histone h3k9cr binding); 103 (histone h3k9cr binding); 375 (kmt2a/mll1 fusion point (in acute myeloid leukemia patient co)); 481 (kmt2a/mll1 fusion point (in acute myeloid leukemia patient f1))

Post-translational modifications (6): 288, 294, 412, 419, 483, 339

Mutagenesis-validated functional residues (11):

Position	Phenotype
28	decreased binding to crotonylated histone h3. decreased binding to acetylated histone h3.
56	decreased binding to crotonylated histone h3. decreased binding to acetylated histone h3.
58	decreased binding to crotonylated histone h3. decreased binding to acetylated histone h3.
59	strongly decreased binding to crotonylated histone h3. decreased binding to acetylated histone h3.
61–67	decreased dna-binding.
77	decreased binding to crotonylated histone h3. decreased binding to acetylated histone h3.
78–79	binds equally well acetylated and crotonylated histone h3.
78	strongly decreased binding to crotonylated histone h3. decreased binding to acetylated histone h3.
78	does not affect ability to discriminate between acetylated and crotonylated histone h3.
81	decreased binding to acetylated histone h3.
103	decreased binding to acetylated histone h3.

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-112382	Formation of RNA Pol II elongation complex
R-HSA-674695	RNA Polymerase II Pre-transcription Events
R-HSA-75955	RNA Polymerase II Transcription Elongation
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)

MSigDB gene sets: 371 (showing top): GGGACCA_MIR133A_MIR133B, VERHAAK_AML_WITH_NPM1_MUTATED_DN, GOBP_HEMATOPOIETIC_PROGENITOR_CELL_DIFFERENTIATION, BENPORATH_ES_WITH_H3K27ME3, GOBP_NON_CANONICAL_WNT_SIGNALING_PATHWAY, AREB6_03, GOZGIT_ESR1_TARGETS_DN, GOBP_REGULATION_OF_NON_CANONICAL_WNT_SIGNALING_PATHWAY, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, MEF2_02, GOBP_REGULATION_OF_WNT_SIGNALING_PATHWAY, ACEVEDO_LIVER_CANCER_WITH_H3K27ME3_UP, GRAHAM_CML_QUIESCENT_VS_NORMAL_QUIESCENT_DN, GOBP_HEMATOPOIETIC_STEM_CELL_DIFFERENTIATION

GO Biological Process (11): sodium ion transport (GO:0006814), segment specification (GO:0007379), anterior/posterior pattern specification (GO:0009952), gene expression (GO:0010467), positive regulation of DNA-templated transcription (GO:0045893), hematopoietic stem cell differentiation (GO:0060218), negative regulation of canonical Wnt signaling pathway (GO:0090090), regulation of chromatin organization (GO:1902275), regulation of stem cell division (GO:2000035), positive regulation of Wnt signaling pathway, planar cell polarity pathway (GO:2000096), chromatin organization (GO:0006325)

GO Molecular Function (9): DNA binding (GO:0003677), chromatin binding (GO:0003682), histone binding (GO:0042393), molecular adaptor activity (GO:0060090), modification-dependent protein binding (GO:0140030), histone H3K18ac reader activity (GO:0140044), histone H3K9ac reader activity (GO:0140072), histone H3K27ac reader activity (GO:0140119), protein binding (GO:0005515)

GO Cellular Component (6): nucleus (GO:0005634), nucleoplasm (GO:0005654), chromosome (GO:0005694), cytosol (GO:0005829), transcription elongation factor complex (GO:0008023), extracellular exosome (GO:0070062)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
RNA Polymerase II Transcription	2
RNA Polymerase II Transcription Elongation	1
Gene expression (Transcription)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
binding	3
histone H3 reader activity	3
protein binding	2
cellular anatomical structure	2
metal ion transport	1
pattern specification process	1
segmentation	1
regionalization	1
macromolecule biosynthetic process	1
DNA-templated transcription	1
regulation of DNA-templated transcription	1
positive regulation of RNA biosynthetic process	1
hematopoietic progenitor cell differentiation	1
stem cell differentiation	1
negative regulation of Wnt signaling pathway	1
canonical Wnt signaling pathway	1
regulation of canonical Wnt signaling pathway	1
chromatin organization	1
regulation of cellular component organization	1
stem cell division	1
regulation of cell division	1
Wnt signaling pathway, planar cell polarity pathway	1
positive regulation of non-canonical Wnt signaling pathway	1
regulation of Wnt signaling pathway, planar cell polarity pathway	1
cellular component organization	1
nucleic acid binding	1
molecular_function	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
intracellular membraneless organelle	1
cytoplasm	1
nucleoplasm	1
nuclear protein-containing complex	1
extracellular vesicle	1

Protein interactions and networks

STRING

2114 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MLLT3	AFF1	P51825	999
MLLT3	ELL	P55199	998
MLLT3	AFF4	Q9UHB7	994
MLLT3	ELL2	O00472	993
MLLT3	MLLT10	P55197	993
MLLT3	DOT1L	Q8TEK3	990
MLLT3	MLLT1	Q03111	983
MLLT3	MLLT6	P55198	965
MLLT3	KMT2A	Q03164	964
MLLT3	CCNT1	O60563	929
MLLT3	H3-3A	P06351	909
MLLT3	H3C14	Q71DI3	909
MLLT3	H3-5	Q6NXT2	909
MLLT3	H3C1	P02295	909
MLLT3	H3-4	Q16695	909
MLLT3	H3-7	Q5TEC6	909

IntAct

133 interactions, top by confidence:

A	B	Type	Score
CDK9	CCNT1	psi-mi:“MI:0914”(association)	0.980
EAF1	ELL2	psi-mi:“MI:0914”(association)	0.840
MLLT3	DOT1L	psi-mi:“MI:0915”(physical association)	0.820
MLLT3	DOT1L	psi-mi:“MI:0407”(direct interaction)	0.820
DOT1L	MLLT3	psi-mi:“MI:0914”(association)	0.820
DOT1L	MLLT3	psi-mi:“MI:0915”(physical association)	0.820
MLLT3	FAM9A	psi-mi:“MI:0915”(physical association)	0.740
MLLT3	AFF1	psi-mi:“MI:0407”(direct interaction)	0.730
MLLT3	AFF1	psi-mi:“MI:0915”(physical association)	0.730
AFF4	ELL2	psi-mi:“MI:0914”(association)	0.730
MLLT3	CDK9	psi-mi:“MI:0914”(association)	0.730
CDK9	AIP	psi-mi:“MI:0914”(association)	0.730
MLLT3	ALKBH4	psi-mi:“MI:0915”(physical association)	0.680
ALKBH4	MLLT3	psi-mi:“MI:0403”(colocalization)	0.680
MLLT3	MIIP	psi-mi:“MI:0915”(physical association)	0.670
MLLT3	APPBP2	psi-mi:“MI:0915”(physical association)	0.670
ELL3	CCNT1	psi-mi:“MI:0914”(association)	0.640
EXOSC3	MTREX	psi-mi:“MI:0914”(association)	0.640

BioGRID (210): MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), APPBP2 (Two-hybrid), MLLT3 (Two-hybrid), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS), MLLT3 (Affinity Capture-MS)

ESM2 similar proteins: A0A1S3XQD6, A0A1S4AX27, A1A5I1, A2AR02, A6QLS2, B0BN49, G2TRQ9, O14256, O55035, P11387, P30189, P41512, P42568, Q04750, Q07050, Q13427, Q27450, Q3KPW4, Q4V9W2, Q505I5, Q59LQ5, Q5BKY9, Q5R8J6, Q5RJP9, Q5VTL8, Q5XHJ5, Q5ZLM8, Q6AXY7, Q6BNE1, Q6NQD9, Q6NWI1, Q751P0, Q7YR26, Q80SY5, Q8GWY0, Q8N9E0, Q8N9Q2, Q8R0F5, Q95KF9, Q96N46

Diamond homologs: A2AM29, F4IPK2, O94436, O95619, P35189, P42568, P53930, Q03111, Q4I7S1, Q4PFI5, Q4WPM8, Q59LC9, Q5BC71, Q6CIV8, Q6FXM4, Q755P0, Q9CR11, Q9FH40, P0CM08, P0CM09, Q10319, Q6CF24, Q7RZK7, Q99314, Q3TUF7, Q9ULM3

SIGNOR signaling

4 interactions.

A	Effect	B	Mechanism
MLLT3	“down-regulates quantity by repression”	SCNN1A	“transcriptional regulation”
MLL-AF4	“down-regulates quantity”	MLLT3	relocalization
P-TEFb	“down-regulates quantity by destabilization”	MLLT3	phosphorylation
SGK1	“down-regulates activity”	MLLT3	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 93 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
Formation of RNA Pol II elongation complex	7	21.2×	4e-06
RNA Polymerase II Transcription Elongation	7	21.2×	4e-06
SUMOylation of transcription cofactors	5	19.0×	5e-04
RNA Polymerase II Pre-transcription Events	8	17.2×	4e-06
Neurexins and neuroligins	5	15.4×	1e-03
RNA polymerase II transcribes snRNA genes	6	14.5×	3e-04

GO biological processes:

GO term	Partners	Fold	FDR
actomyosin structure organization	5	32.7×	9e-05
transcription elongation by RNA polymerase II	6	30.9×	1e-05
positive regulation of transcription elongation by RNA polymerase II	7	24.5×	9e-06

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: ambiguous (mixed evidence) across 1 cancer types — MEL.

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	62
Likely benign	10
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

5451 predictions. Top by Δscore:

Variant	Effect	Δscore
9:20360837:TAACT:T	acceptor_gain	1.0000
9:20363472:TCAC:T	donor_loss	1.0000
9:20363473:CA:C	donor_loss	1.0000
9:20363474:A:AC	donor_gain	1.0000
9:20363474:AC:A	donor_gain	1.0000
9:20363475:C:CG	donor_gain	1.0000
9:20363475:CC:C	donor_gain	1.0000
9:20363475:CCT:C	donor_gain	1.0000
9:20363475:CCTG:C	donor_gain	1.0000
9:20363603:GACC:G	acceptor_loss	1.0000
9:20363606:C:CC	acceptor_gain	1.0000
9:20363607:T:G	acceptor_loss	1.0000
9:20364231:CAGCA:C	acceptor_gain	1.0000
9:20364235:A:C	acceptor_gain	1.0000
9:20364237:G:C	acceptor_gain	1.0000
9:20413717:TCAC:T	donor_loss	1.0000
9:20413718:CA:C	donor_loss	1.0000
9:20413719:A:AC	donor_gain	1.0000
9:20413719:ACAT:A	donor_gain	1.0000
9:20413720:C:CA	donor_gain	1.0000
9:20413720:C:G	donor_loss	1.0000
9:20413720:CAT:C	donor_gain	1.0000
9:20413720:CATC:C	donor_gain	1.0000
9:20413720:CATCA:C	donor_gain	1.0000
9:20414425:CCT:C	acceptor_loss	1.0000
9:20414426:C:CA	acceptor_loss	1.0000
9:20414426:C:CC	acceptor_gain	1.0000
9:20448116:CACTT:C	donor_loss	1.0000
9:20448117:ACTTA:A	donor_loss	1.0000
9:20448118:CTTA:C	donor_loss	1.0000

AlphaMissense

3878 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
9:20346474:T:G	Q559P	1.000
9:20346477:A:C	L558R	1.000
9:20346477:A:G	L558P	1.000
9:20346477:A:T	L558Q	1.000
9:20346486:A:T	V555D	1.000
9:20346498:T:A	D551V	1.000
9:20346501:A:C	L550R	1.000
9:20346501:A:G	L550P	1.000
9:20346501:A:T	L550Q	1.000
9:20346510:A:C	L547R	1.000
9:20346510:A:G	L547P	1.000
9:20346510:A:T	L547H	1.000
9:20346512:A:C	D546E	1.000
9:20346512:A:T	D546E	1.000
9:20346513:T:A	D546V	1.000
9:20346513:T:C	D546G	1.000
9:20346513:T:G	D546A	1.000
9:20346515:A:C	F545L	1.000
9:20346515:A:T	F545L	1.000
9:20346516:A:C	F545C	1.000
9:20346516:A:G	F545S	1.000
9:20346517:A:C	F545V	1.000
9:20346517:A:G	F545L	1.000
9:20346517:A:T	F545I	1.000
9:20346519:T:A	D544V	1.000
9:20346519:T:C	D544G	1.000
9:20346521:A:C	F543L	1.000
9:20346521:A:T	F543L	1.000
9:20346522:A:C	F543C	1.000
9:20346522:A:G	F543S	1.000

dbSNP variants (sampled 300 via entrez): RS1000014419 (9:20619530 A>C), RS1000015841 (9:20563294 A>C,G), RS1000026164 (9:20599336 G>A), RS1000041636 (9:20593431 A>G), RS1000045910 (9:20554060 T>G), RS1000075457 (9:20371831 G>A), RS1000084346 (9:20557262 T>C), RS1000089406 (9:20402198 A>T), RS1000091878 (9:20408028 T>G), RS1000113860 (9:20445191 C>T), RS1000114868 (9:20480950 T>A), RS1000122390 (9:20552889 A>C,G), RS1000129237 (9:20608794 CATAAT>C), RS1000129392 (9:20385593 G>A), RS1000137767 (9:20521819 A>C)

Disease associations

OMIM: gene MIM:159558 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

11 associations (top):

Study	Trait	p-value
GCST002979_1	Response to montelukast in asthma (change in FEV1)	2.000000e-09
GCST006061_86	Atrial fibrillation	9.000000e-09
GCST007267_126	Systolic blood pressure	2.000000e-10
GCST008058_255	Estimated glomerular filtration rate	7.000000e-13
GCST008059_172	Estimated glomerular filtration rate	2.000000e-13
GCST010599_11	Dietary fat liking	1.000000e-06
GCST012441_1	Glutathione peroxidase in non-alcoholic fatty liver disease x mastiha supplementation interaction	1.000000e-09
GCST90002383_511	Hematocrit	1.000000e-09
GCST90002384_257	Hemoglobin	2.000000e-09
GCST90002396_402	Mean reticulocyte volume	1.000000e-09
GCST90002401_477	Platelet distribution width	2.000000e-15

EFO canonical traits (8, from GWAS)

EFO ID	Trait name
EFO:0005921	FEV change measurement
EFO:0006335	systolic blood pressure
EFO:0010816	dietary fat liking measurement
EFO:0600067	mastiha supplement exposure measurement
EFO:0004348	hematocrit
EFO:0004509	hemoglobin measurement
EFO:0010701	mean reticulocyte volume
EFO:0007984	platelet component distribution width

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4295761 (SINGLE PROTEIN)

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

PharmGKB clinical annotations

2 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs10964552	Efficacy	3	cisplatin	Urinary Bladder Neoplasms
rs6475448	Efficacy	3	montelukast	Asthma

PharmGKB variants

3 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs6475448	MLLT3	3	0.00	1	montelukast
rs12350051	MLLT3		0.00	0
rs10964552	MLLT3	3	2.25	1	cisplatin

ChEMBL bioactivities

95 potent at pChembl≥5 of 103 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.05	Ki	9	nM	CHEMBL4206834
8.05	Ki	9	nM	CHEMBL5198951
8.05	Ki	9	nM	CHEMBL5187149
8.00	Ki	10	nM	CHEMBL4204744
7.89	Ki	13	nM	CHEMBL4211204
7.89	Ki	13	nM	CHEMBL5197715
7.82	Kd	15	nM	CHEMBL4204744
7.82	Ki	15	nM	CHEMBL5184570
7.77	Ki	17	nM	CHEMBL5206253
7.72	Ki	19	nM	CHEMBL5199592
7.70	Ki	20	nM	CHEMBL4209820
7.70	Ki	20	nM	CHEMBL4216416
7.66	Ki	22	nM	CHEMBL5203898
7.64	Ki	23	nM	CHEMBL4211714
7.64	Ki	23	nM	CHEMBL5208460
7.54	Ki	29	nM	CHEMBL5190103
7.50	Ki	32	nM	CHEMBL5207031
7.30	Ki	50	nM	CHEMBL4216933
7.24	IC50	57	nM	CHEMBL4206834
7.24	Ki	57	nM	CHEMBL4211962
7.24	Ki	57	nM	CHEMBL4216170
7.12	Kd	76	nM	CHEMBL4752253
7.09	IC50	82	nM	CHEMBL4211204
6.96	Kd	110	nM	CHEMBL4752253
6.92	IC50	120	nM	CHEMBL4216416
6.92	IC50	120	nM	CHEMBL5429859
6.89	Ki	130	nM	CHEMBL4209508
6.85	IC50	140	nM	CHEMBL4209820
6.83	IC50	149	nM	CHEMBL4211714
6.80	Ki	160	nM	CHEMBL4204942
6.80	Ki	160	nM	CHEMBL4204545
6.80	Ki	160	nM	CHEMBL4210431
6.80	Ki	160	nM	CHEMBL5187921
6.80	IC50	160	nM	CHEMBL4752253
6.77	Ki	170	nM	CHEMBL4210431
6.75	Ki	180	nM	CHEMBL4204647
6.72	Ki	190	nM	CHEMBL4209087
6.70	IC50	200	nM	CHEMBL5421606
6.60	Ki	250	nM	CHEMBL4213382
6.59	IC50	254	nM	CHEMBL4800073
6.55	Ki	280	nM	CHEMBL4212941
6.52	Ki	300	nM	CHEMBL4216206
6.47	IC50	341	nM	CHEMBL4216933
6.43	IC50	372	nM	CHEMBL4211962
6.43	IC50	369	nM	CHEMBL4216170
6.43	Kd	370	nM	CHEMBL4850575
6.39	Ki	410	nM	CHEMBL4217882
6.39	IC50	410	nM	CHEMBL4850575
6.30	IC50	500	nM	CHEMBL5416331
6.30	IC50	500	nM	CHEMBL5398308

PubChem BioAssay actives

90 with measured affinity, of 124 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
(2S)-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-1-[(2S)-2-[1-(cyclohexylmethyl)-4-phenylimidazol-2-yl]pyrrolidin-1-yl]-3-cyclopentyl-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-1-benzoylpyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0090	uM
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-3-cyclopentyl-1-oxo-1-[[(1S)-1-(4-phenyl-1H-benzimidazol-2-yl)ethyl]amino]propan-2-yl]amino]-3-(methylamino)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-1-(4-methylpentanoyl)pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0090	uM
(2S)-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-oxo-1-[[(1S)-1-(4-phenyl-1H-benzimidazol-2-yl)ethyl]amino]propan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-1-(4-methylpentanoyl)pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0090	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[6-[5-[(3aR,4S,6aS)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]hexanoylamino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-aminopropanoyl]amino]-3-cyclopentylpropanoyl]-N-[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0100	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-1-[(2S)-2-[1-(cyclohexylmethyl)-4-phenylimidazol-2-yl]pyrrolidin-1-yl]-3-cyclopentyl-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0130	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-oxo-1-[[(1S)-2-phenyl-1-(4-phenyl-1H-benzimidazol-2-yl)ethyl]amino]propan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0130	uM
(2S)-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-oxo-1-[[(1S)-1-(4-phenyl-1H-benzimidazol-2-yl)ethyl]amino]propan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-1-benzoylpyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0150	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-oxo-1-[[(1S)-1-(4-phenyl-1H-benzimidazol-2-yl)ethyl]amino]propan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0170	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-[[(1S)-3-methyl-1-(4-phenyl-1H-benzimidazol-2-yl)butyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0190	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0200	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-aminopropanoyl]amino]-3-cyclopentylpropanoyl]-N-[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0200	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-oxo-1-[(2S)-2-(4-phenyl-1H-benzimidazol-2-yl)pyrrolidin-1-yl]propan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0220	uM
(2S)-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-1-[(2S)-2-[1-(cyclohexylmethyl)-4-phenylimidazol-2-yl]pyrrolidin-1-yl]-3-cyclopentyl-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-1-(4-methylpentanoyl)pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0230	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-[[(1S,2S)-2-methyl-1-(4-phenyl-1H-benzimidazol-2-yl)butyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0230	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-[[(1S)-2-methyl-1-(4-phenyl-1H-benzimidazol-2-yl)propyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0290	uM
(2S)-1-benzoyl-N-[(2S)-1-[[(2S)-1-[[(2S)-3-cyclopentyl-1-oxo-1-[[(1S)-1-(4-phenyl-1H-benzimidazol-2-yl)ethyl]amino]propan-2-yl]amino]-3-(methylamino)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0320	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-[(2S)-2-(1-ethyl-4-phenylimidazol-2-yl)pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0500	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-[(2S)-2-(1-methyl-4-phenylimidazol-2-yl)pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0570	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-3-amino-1-[[(2S)-3-cyclopentyl-1-oxo-1-[(2S)-2-(4-phenyl-1-propan-2-ylimidazol-2-yl)pyrrolidin-1-yl]propan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0570	uM
N-[(1R)-2,3-dihydro-1H-inden-1-yl]-5-[4-(dimethylcarbamoyl)-3-hydroxyphenyl]-1,2-oxazole-3-carboxamide	2004075: Binding affinity to MLLT3 YD domain (unknown origin) assessed as dissociation constant by isothermal calorimetry assay	kd	0.0760	uM
N-cyclopentyl-5-[4-(dimethylcarbamoyl)-3-hydroxyphenyl]-1,2-oxazole-3-carboxamide	2004067: Inhibition of MLLT3 YD domain (unknown origin) assessed as disruption of histone peptide binding using histone peptide as substrate by HTRF assay	ic50	0.1200	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-cyclopentylpropanoyl]-N-[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.1300	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.1600	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.1600	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.1600	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S,3R)-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1911456: Binding affinity to MBP-tagged human recombinant AF9 (487 to 568 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.1600	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-cyclohexylpropanoyl]-N-[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.1800	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S,3S)-1-[[(2S)-3-amino-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.1900	uM
N-cyclopentyl-5-(5-hydroxyquinolin-7-yl)-1,2-oxazole-3-carboxamide	2004067: Inhibition of MLLT3 YD domain (unknown origin) assessed as disruption of histone peptide binding using histone peptide as substrate by HTRF assay	ic50	0.2000	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S,3S)-1-[[(2S)-1-[[(1S)-1-cyclopentyl-2-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.2500	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]-N-[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.2800	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.3000	uM
benzyl N-[(7R,10S,13S,16S)-2-amino-7-[[(2S)-1-amino-6-(1,3-oxazole-5-carbonylamino)-1-oxohexan-2-yl]carbamoyl]-13-[(1S)-1-hydroxyethyl]-10-methyl-9,12,15-trioxo-1,3,8,11,14-pentazacycloicos-2-en-16-yl]carbamate	1777533: Binding affinity to AF9 YEATS domain (1 to 138 residues) (unknown origin) by isothermal titration calorimetry	kd	0.3700	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]-N-[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.4100	uM
N-cyclopentyl-1-(3-hydroxyphenyl)imidazole-4-carboxamide	2004067: Inhibition of MLLT3 YD domain (unknown origin) assessed as disruption of histone peptide binding using histone peptide as substrate by HTRF assay	ic50	0.5000	uM
5-(4-chloro-3-hydroxyphenyl)-N-cyclopentyl-1,2-oxazole-3-carboxamide	2004067: Inhibition of MLLT3 YD domain (unknown origin) assessed as disruption of histone peptide binding using histone peptide as substrate by HTRF assay	ic50	0.5000	uM
1-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	2004087: Binding affinity to MLLT3 in human HEK293 cells by NanoBRET assay	ic50	0.6000	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S,3S)-1-[[(2S)-1-[[(1S)-1-cyclohexyl-2-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.6200	uM
N-cyclopentyl-5-(3-hydroxyphenyl)-1,2-oxazole-3-carboxamide	2004067: Inhibition of MLLT3 YD domain (unknown origin) assessed as disruption of histone peptide binding using histone peptide as substrate by HTRF assay	ic50	0.6300	uM
N-[[4-[[(5-fluoropyrimidin-2-yl)amino]methyl]phenyl]methyl]-[1,2,4]triazolo[4,3-a]pyridine-6-carboxamide	1751797: Inhibition of human His-AF9 YEATS domain and biotinylated H3K9ac peptide interaction by AlphaScreen assay	ic50	0.7290	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-naphthalen-2-ylpropanoyl]-N-[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.7300	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-3-cyclopropyl-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.7800	uM
benzyl N-[(7R,10S,13S,16S)-10-[4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-6-aminohexanoyl]amino]-6-aminohexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-amino-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]butyl]-7-[[(2S)-1-amino-6-(1,3-oxazole-5-carbonylamino)-1-oxohexan-2-yl]carbamoyl]-13-[(1S)-1-hydroxyethyl]-2-imino-9,12,15-trioxo-1,3,8,11,14-pentazacycloicos-16-yl]carbamate	1777533: Binding affinity to AF9 YEATS domain (1 to 138 residues) (unknown origin) by isothermal titration calorimetry	kd	0.8000	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.8300	uM
N-[[4-(azetidin-1-ylmethyl)phenyl]methyl]-[1,2,4]triazolo[4,3-a]pyridine-6-carboxamide	1751797: Inhibition of human His-AF9 YEATS domain and biotinylated H3K9ac peptide interaction by AlphaScreen assay	ic50	0.9840	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	1.1600	uM
(2S)-1-[(2S)-2-acetamido-4-methylpentanoyl]-N-[(2S)-3-cyclobutyl-1-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-(dimethylamino)-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]pyrrolidine-2-carboxamide	1387576: Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	1.3100	uM
1-[1-[(2S)-2-(4-chlorophenyl)-2-hydroxyethyl]piperidin-4-yl]-N-ethyl-2-oxo-3H-benzimidazole-5-carboxamide	1964937: Binding affinity to human his-tagged recombinant YEATS3 expressed in Escherichia coli assessed as inhibition constant using biotin tagged lysine 27-crotonylated histone H3 peptide as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by FRET analysis	ki	1.5000	uM
N-[(4-methylsulfanylphenyl)methyl]-[1,2,4]triazolo[4,3-a]pyridine-6-carboxamide	1751797: Inhibition of human His-AF9 YEATS domain and biotinylated H3K9ac peptide interaction by AlphaScreen assay	ic50	1.8500	uM
N-cyclopentyl-1-(3-hydroxyphenyl)pyrazole-4-carboxamide	2004067: Inhibition of MLLT3 YD domain (unknown origin) assessed as disruption of histone peptide binding using histone peptide as substrate by HTRF assay	ic50	2.4000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, increases expression, affects expression	8
Benzo(a)pyrene	decreases expression, affects methylation	3
Cyclosporine	decreases expression	3
trichostatin A	affects expression, increases expression	2
Acetaminophen	affects expression, decreases expression	2
Air Pollutants	decreases expression, increases abundance	2
aristolochic acid I	decreases expression	1
GSK-J4	increases expression	1
FR900359	decreases phosphorylation	1
dicrotophos	decreases expression	1
methylmercuric chloride	decreases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases methylation	1
lead acetate	increases expression, affects cotreatment	1
zinc protoporphyrin	affects cotreatment, increases expression	1
perfluorooctanoic acid	increases expression	1
benzo(e)pyrene	affects methylation	1
aflatoxin B2	decreases methylation	1
nickel sulfate	decreases expression	1
perfluorooctane sulfonic acid	increases expression	1
2-palmitoylglycerol	increases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
dorsomorphin	affects cotreatment, increases expression	1
Sunitinib	decreases expression	1
Atrazine	increases expression	1
Carbamazepine	affects expression	1
Doxorubicin	decreases expression	1
Estradiol	affects expression	1
Melphalan	decreases expression	1
Methapyrilene	affects methylation	1

ChEMBL screening assays

41 unique, capped per target: 41 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4202266	Binding	Displacement of N-Flu-DOT1L from MBP-tagged AF9 (unknown origin) (487 to 568 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	Peptidomimetics for Targeting Protein-Protein Interactions between DOT1L and MLL Oncofusion Proteins AF9 and ENL. — ACS Med Chem Lett

Cellosaurus cell lines

496 cell lines: 496 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_0006	THP-1	Cancer cell line	Male
CVCL_0R21	THP-1/DC-SIGN	Cancer cell line	Male
CVCL_0R25	THP-1(NCI)	Cancer cell line	Male
CVCL_0R26	THP-1(NCI)/DC-SIGN	Cancer cell line	Male
CVCL_1426	Mono-Mac-6	Cancer cell line	Male
CVCL_1609	NOMO-1	Cancer cell line	Female
CVCL_2119	MOLM-13	Cancer cell line	Male
CVCL_3077	NOMO-1/ADM	Cancer cell line	Female
CVCL_3078	NOMO-1s	Cancer cell line	Female
CVCL_3426	THP-1h	Cancer cell line	Male

Clinical trials (associated diseases)

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