MLLT1

Summary

MLLT1 (MLLT1 super elongation complex subunit, HGNC:7134) is a protein-coding gene on chromosome 19p13.3, encoding Protein ENL (Q03111). 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.

Predicted to enable chromatin binding activity and lysine-acetylated histone binding activity. Predicted to be involved in positive regulation of DNA-templated transcription. Predicted to act upstream of or within negative regulation of protein kinase activity. Located in cytosol; fibrillar center; and nucleoplasm. Part of transcription elongation factor complex.

Source: NCBI Gene 4298 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 80 total — 1 likely-pathogenic
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer driver (intOGen): activating (oncogene-like) across 1 cancer types
• MANE Select transcript: NM_005934

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:7134
Approved symbol	MLLT1
Name	MLLT1 super elongation complex subunit
Location	19p13.3
Locus type	gene with protein product
Status	Approved
Aliases	ENL, LTG19, YEATS1
Ensembl gene	ENSG00000130382
Ensembl biotype	protein_coding
OMIM	159556
Entrez	4298

Gene structure

Transcript identifiers

Ensembl transcripts: 6 — 5 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000252674, ENST00000585588, ENST00000587473, ENST00000867663, ENST00000943586, ENST00000943587

RefSeq mRNA: 1 — MANE Select: NM_005934 NM_005934

CCDS: CCDS12160

Canonical transcript exons

ENST00000252674 — 12 exons

Exon	Start	End
ENSE00000666098	6262228	6262310
ENSE00000666100	6230570	6230713
ENSE00000666102	6226977	6227102
ENSE00000857471	6222121	6222684
ENSE00001052838	6217954	6218041
ENSE00001157759	6270579	6270759
ENSE00001295439	6279773	6279975
ENSE00001765706	6210381	6213170
ENSE00003648915	6213939	6214038
ENSE00003657210	6213337	6213408
ENSE00003669438	6216405	6216513
ENSE00003680130	6213726	6213797

Expression profiles

Bgee: expression breadth ubiquitous, 259 present calls, max score 97.85.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 24.8553 / max 288.7524, expressed in 1806 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
178612	20.4238	1802
178614	2.4251	1490
178613	0.8379	585
178607	0.6252	161
178608	0.5433	182

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
pancreatic ductal cell	CL:0002079	97.85	silver quality
cardiac muscle of right atrium	UBERON:0003379	97.83	gold quality
placenta	UBERON:0001987	97.21	gold quality
right uterine tube	UBERON:0001302	96.37	gold quality
right hemisphere of cerebellum	UBERON:0014890	95.29	gold quality
left ventricle myocardium	UBERON:0006566	95.02	silver quality
tibialis anterior	UBERON:0001385	94.77	silver quality
cerebellar hemisphere	UBERON:0002245	94.70	gold quality
cerebellar cortex	UBERON:0002129	94.63	gold quality
nucleus accumbens	UBERON:0001882	94.51	gold quality
right frontal lobe	UBERON:0002810	94.28	gold quality
ventricular zone	UBERON:0003053	94.17	gold quality
decidua	UBERON:0002450	94.16	gold quality
oocyte	CL:0000023	93.95	gold quality
lower lobe of lung	UBERON:0008949	93.73	gold quality
left uterine tube	UBERON:0001303	93.70	gold quality
upper arm skin	UBERON:0004263	93.69	silver quality
cortical plate	UBERON:0005343	93.59	gold quality
postcentral gyrus	UBERON:0002581	93.57	gold quality
cerebellum	UBERON:0002037	93.41	gold quality
right ovary	UBERON:0002118	93.23	gold quality
amygdala	UBERON:0001876	93.22	gold quality
parietal lobe	UBERON:0001872	93.02	gold quality
left ovary	UBERON:0002119	93.00	gold quality
endocervix	UBERON:0000458	92.86	gold quality
apex of heart	UBERON:0002098	92.82	gold quality
hypothalamus	UBERON:0001898	92.68	gold quality
ganglionic eminence	UBERON:0004023	92.62	gold quality
Brodmann (1909) area 9	UBERON:0013540	92.57	gold quality
ileal mucosa	UBERON:0000331	92.39	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-MTAB-6701	yes	133.37
E-ANND-3	yes	10.55
E-MTAB-7249	no	31.60

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): EZH2, KMT2A

miRNA regulators (miRDB)

143 targeting MLLT1, 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-4481	100.00	66.42	1669
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-6798-5P	100.00	65.77	699
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-513B-5P	99.99	69.96	2150
HSA-MIR-4745-5P	99.98	65.95	1028
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-495-3P	99.96	72.81	4197
HSA-MIR-146A-5P	99.96	68.93	988
HSA-MIR-146B-5P	99.96	69.13	977
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-185-3P	99.95	67.01	1743
HSA-MIR-96-5P	99.95	72.80	2140
HSA-MIR-7153-5P	99.94	68.89	1006
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-22-3P	99.93	68.13	917
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394
HSA-MIR-8087	99.90	69.55	1351
HSA-MIR-4731-5P	99.89	67.23	2537

Literature-anchored findings (GeneRIF, showing 19)

• ENL chromatin-remodeling complexes contain a mixed-lineage leukemia chromosomal translocation partner. (PMID:12665591)
• determination of the relative positions of MLL, AF4 and ENL genes, in two lymphoblastic and two myeloid human cell lines (PMID:16433901)
• In acute leukemias with a t(11:19) translocation, 50% of the analyzed breakpoints were within the MLLT1 gene introns. The MLL gene was fused to the intact MLLT1 gene by transcriptional readthrough & a splice event, or by trans-splicing. (PMID:17252016)
• Three-way translocation involving MLL, MLLT1, and a novel third partner, NRXN1, in a patient with acute lymphoblastic leukemia and t(2;19;11) (p12;p13.3;q23). (PMID:20113834)
• Data from a follow-up study in Rome suggest a particularly favorable prognosis for patients with acute lymphoblastic leukemia expressing the MLL/ENL fusion gene. (PMID:21953510)
• MLL-ENL Interaction with CBX8 Is Required for Efficient Transformation. (PMID:23623499)
• MLL-ENL dysregulated the proliferative and repopulating capacity of hematopoietic stem cells. (PMID:25456127)
• Novel splice isoform of Mllt1 is documented and confirmed that both Mllt1 mRNA isoforms are translated. The data support that MLLT1 protein isoforms display distinct stage-specific expression during spermiogenesis and adult tissues. (PMID:25481096)
• AF9 and its homolog ENL directly interact with AF4. (PMID:25509985)
• Data suggest that AT mutated protein ATM-dependent phosphorylation of ENL (MLLT1) protein functions as switch from elongation to Polycomb-mediated repression to preserve genome integrity. (PMID:25921070)
• Recurrent mutations within Wilms tumours involve the highly conserved YEATS domain of MLLT1. (PMID:26635203)
• data identify ENL as a histone acetylation reader that regulates oncogenic transcriptional programs in acute myeloid leukaemia, and suggest that displacement of ENL from chromatin may be a promising epigenetic therapy, alone or in combination with BET inhibitors, for aggressive leukaemia (PMID:28241141)
• This review will not only provide a fundamental understanding of the structure and function of ENL and update on the roles of ENL in acute myeloid leukemia, but also the development of new therapeutic strategies (PMID:30066088)
• Our findings show that the efficiency of MLL-ENL-driven AML initiation changes through the course of pre- and postnatal development, and developmental programs can be manipulated to impede transformation. (PMID:31405949)
• Structure and Inhibitor Binding Characterization of Oncogenic MLLT1 Mutants. (PMID:33749253)
• 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)
• KAT6A and ENL Form an Epigenetic Transcriptional Control Module to Drive Critical Leukemogenic Gene-Expression Programs. (PMID:34853079)
• The ENL YEATS epigenetic reader domain critically links MLL-ENL to leukemic stem cell frequency in t(11;19) Leukemia. (PMID:36435883)
• Circvrk1 downregulation attenuates brain microvascular endothelial cell damage induced by oxygen-glucose deprivation through modulating the miR-150-5p/MLLT1 axis. (PMID:36735043)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	mllt1a	ENSDARG00000043185
mus_musculus	Mllt1	ENSMUSG00000024212
rattus_norvegicus	Mllt1	ENSRNOG00000048736
drosophila_melanogaster	ear	FBGN0026441

Paralogs (2): YEATS2 (ENSG00000163872), MLLT3 (ENSG00000171843)

Protein

Protein identifiers

Protein ENL — Q03111 (reviewed: Q03111)

Alternative names: Eleven-nineteen-leukeumia, YEATS domain-containing protein 1

All UniProt accessions (2): Q03111, A0AAQ5BI09

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 acetylated and crotonylated histones, with a preference for histones that are crotonylated. Has a slightly higher affinity for binding histone H3 crotonylated at ‘Lys-27’ (H3K27cr) than ‘Lys-20’ (H3K9cr20). May play a role in leukemogenic gene transcription. Acts as a key chromatin reader in acute myeloid leukemia by recognizing and binding to acetylated histones via its YEATS domain, thereby regulating oncogenic 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 ALKBH4. Interacts with acetylated or crotonylated KAT6A/MOZ; the interaction is direct. Component of a SWI/SNF-like EBAFb complex, at least composed of SMARCA4/BRG1/BAF190A, SMARCB1/BAF47/SNF5, ACTL6A/BAF53A, SMARCE1/BAF57, SMARCD1/BAF60A, SMARCD2/BAF60B, SMARCC1/BAF155, SMARCC2/BAF170, ARID1B/BAF250B, MLLT1/ENL and actin.

Subcellular location. Nucleus.

Disease relevance. A chromosomal aberration involving MLLT1 is associated with acute leukemias. Translocation t(11;19)(q23;p13.3) with KMT2A/MLL1. The result is a rogue activator protein.

Activity regulation. Acylated lysine-binding is specifically inhibited by the tripeptide XL-13m, carrying a 2-furancarbonyl side chain, preventing recruitment to chromatin.

Domain organisation. The YEATS domain specifically recognizes and binds acylated histones, with a preference for histones that are crotonylated.

RefSeq proteins (1): NP_005925* (*=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 (40 total): strand 12, compositionally biased region 10, modified residue 6, region of interest 3, cross-link 3, helix 2, chain 1, domain 1, site 1, sequence conflict 1

Structure

Experimental structures (PDB)

26 structures.

PDB	Method	Resolution (Å)
8PJI	X-RAY DIFFRACTION	1.7
6HT0	X-RAY DIFFRACTION	1.8
6T1I	X-RAY DIFFRACTION	1.8
6HQ0	X-RAY DIFFRACTION	1.81
7E7C	X-RAY DIFFRACTION	1.84
6T1M	X-RAY DIFFRACTION	1.85
6HPW	X-RAY DIFFRACTION	1.9
6T1O	X-RAY DIFFRACTION	1.9
7X8G	X-RAY DIFFRACTION	1.91
7B10	X-RAY DIFFRACTION	1.92
6T1N	X-RAY DIFFRACTION	1.95
6T1J	X-RAY DIFFRACTION	1.97
6HPY	X-RAY DIFFRACTION	2
6T1L	X-RAY DIFFRACTION	2
7B0T	X-RAY DIFFRACTION	2.05
6HT1	X-RAY DIFFRACTION	2.1
7X88	X-RAY DIFFRACTION	2.25
6HPX	X-RAY DIFFRACTION	2.3
6HPZ	X-RAY DIFFRACTION	2.3
7X8B	X-RAY DIFFRACTION	2.3
7X8F	X-RAY DIFFRACTION	2.44
9EHI	X-RAY DIFFRACTION	2.6
7E7A	X-RAY DIFFRACTION	2.64
5J9S	X-RAY DIFFRACTION	2.7
7E74	X-RAY DIFFRACTION	2.9
9DUR	ELECTRON MICROSCOPY	2.9

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q03111-F1	65.81	0.36

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): 103 (acylated histone binding)

Post-translational modifications (9): 1, 155, 292, 296, 359, 361, 240, 262, 342

Function

Pathways and Gene Ontology

Reactome pathways

3 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

MSigDB gene sets: 128 (showing top): FONTAINE_PAPILLARY_THYROID_CARCINOMA_UP, MODULE_379, MARTINEZ_RB1_TARGETS_DN, BOYLAN_MULTIPLE_MYELOMA_C_CLUSTER_UP, MODULE_242, GOMF_CHROMATIN_BINDING, MODULE_104, GOCC_NUCLEOLUS, GOCC_TRANSCRIPTION_ELONGATION_FACTOR_COMPLEX, chr19p13, MODULE_7, MODULE_181, TOYOTA_TARGETS_OF_MIR34B_AND_MIR34C, MODULE_41, BYSTRYKH_HEMATOPOIESIS_STEM_CELL_QTL_TRANS

GO Biological Process (1): positive regulation of DNA-templated transcription (GO:0045893)

GO Molecular Function (2): chromatin binding (GO:0003682), protein binding (GO:0005515)

GO Cellular Component (5): fibrillar center (GO:0001650), nucleoplasm (GO:0005654), cytosol (GO:0005829), transcription elongation factor complex (GO:0008023), nucleus (GO:0005634)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
RNA Polymerase II Transcription	2
RNA Polymerase II Transcription Elongation	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
binding	2
DNA-templated transcription	1
regulation of DNA-templated transcription	1
positive regulation of RNA biosynthetic process	1
nucleolus	1
nuclear lumen	1
cytoplasm	1
nucleoplasm	1
nuclear protein-containing complex	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

2124 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MLLT1	AFF1	P51825	999
MLLT1	ELL	P55199	999
MLLT1	ELL2	O00472	995
MLLT1	AFF4	Q9UHB7	995
MLLT1	CCNT1	O60563	984
MLLT1	DOT1L	Q8TEK3	984
MLLT1	MLLT3	P42568	983
MLLT1	MLLT10	P55197	966
MLLT1	CDK9	P50750	964
MLLT1	MLLT6	P55198	949
MLLT1	KMT2A	Q03164	948
MLLT1	BMI1	P35226	882
MLLT1	R4GMX3	R4GMX3	882
MLLT1	AFDN	P55196	874
MLLT1	ELL3	Q9HB65	864

IntAct

107 interactions, top by confidence:

A	B	Type	Score
CDK9	CCNT1	psi-mi:“MI:0914”(association)	0.980
RYBP	BMI1	psi-mi:“MI:0914”(association)	0.850
EAF1	ELL2	psi-mi:“MI:0914”(association)	0.840
DOT1L	MLLT3	psi-mi:“MI:0914”(association)	0.820
AFF4	CCNT1	psi-mi:“MI:0914”(association)	0.810
AFF4	MLLT1	psi-mi:“MI:0915”(physical association)	0.760
AFF4	MLLT1	psi-mi:“MI:0914”(association)	0.760
AFF4	ELL2	psi-mi:“MI:0914”(association)	0.730
CDK9	AIP	psi-mi:“MI:0914”(association)	0.730
MLLT1	DOT1L	psi-mi:“MI:0915”(physical association)	0.680
DOT1L	MLLT1	psi-mi:“MI:0915”(physical association)	0.680
MLLT1	DOT1L	psi-mi:“MI:0914”(association)	0.680
ELL3	CCNT1	psi-mi:“MI:0914”(association)	0.640
YAF2	E2F6	psi-mi:“MI:0914”(association)	0.640
CAMKV	AP3B1	psi-mi:“MI:0914”(association)	0.640
MLLT1	ELL2	psi-mi:“MI:0914”(association)	0.640

BioGRID (226): MLLT1 (Affinity Capture-MS), MLLT1 (Affinity Capture-MS), MLLT1 (Affinity Capture-MS), MLLT1 (Co-fractionation), AFF1 (Affinity Capture-MS), CDK9 (Affinity Capture-MS), RNF2 (Affinity Capture-MS), RPL12 (Affinity Capture-MS), MRPL12 (Affinity Capture-MS), HIST2H2AC (Affinity Capture-MS), H2AFX (Affinity Capture-MS), HIST2H2BE (Affinity Capture-MS), HIST4H4 (Affinity Capture-MS), RNF2 (Affinity Capture-Western), BMI1 (Affinity Capture-Western)

ESM2 similar proteins: A0A0G2L7I0, A0A0R4IWG9, A0JMK9, A5D979, B0BLU1, D3ZVU1, F6UH96, G3X912, O70445, O88700, P54132, P59110, Q03111, Q0VBD2, Q1LVK9, Q22557, Q24558, Q24595, Q28E45, Q5EAW4, Q5I2W8, Q5R1T0, Q5SPR8, Q5XI59, Q6A037, Q6DJS0, Q6INS5, Q6P2L6, Q6XV80, Q6ZPI0, Q71M44, Q7KW09, Q7L590, Q7T308, Q7ZVP1, Q7ZXG4, Q801E2, Q803U7, Q80Z32, Q8AXF4

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

2 interactions.

A	Effect	B	Mechanism
MLLT1	“form complex”	“AEP complex”	binding
P-TEFb	“down-regulates quantity by destabilization”	MLLT1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 78 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	6	20.4×	8e-05
RNA Polymerase II Transcription Elongation	6	20.4×	8e-05
RNA Polymerase II Pre-transcription Events	6	14.5×	4e-04
RNA polymerase II transcribes snRNA genes	5	13.5×	1e-03
mRNA Splicing - Major Pathway	8	7.7×	7e-04
Dengue Virus-Host Interactions	8	6.4×	1e-03

GO biological processes:

GO term	Partners	Fold	FDR
transcription elongation by RNA polymerase II	5	30.4×	3e-04
positive regulation of transcription elongation by RNA polymerase II	5	20.6×	1e-03
chromatin remodeling	7	7.0×	7e-03

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: activating (oncogene-like) across 1 cancer types — WT.

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	1
Uncertain significance	59
Likely benign	2
Benign	1

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
242890	NM_005934.4(MLLT1):c.1418G>A (p.Arg473Gln)	Likely pathogenic

SpliceAI

3214 predictions. Top by Δscore:

Variant	Effect	Δscore
19:6213167:CAAT:C	acceptor_gain	1.0000
19:6213169:ATC:A	acceptor_loss	1.0000
19:6213171:C:CC	acceptor_gain	1.0000
19:6213172:T:C	acceptor_loss	1.0000
19:6213333:ATAC:A	donor_loss	1.0000
19:6213334:TA:T	donor_loss	1.0000
19:6213335:A:T	donor_loss	1.0000
19:6213336:C:CA	donor_loss	1.0000
19:6213336:CCTG:C	donor_gain	1.0000
19:6213404:TAGGC:T	acceptor_gain	1.0000
19:6213405:AGGC:A	acceptor_gain	1.0000
19:6213406:GGC:G	acceptor_gain	1.0000
19:6213407:GC:G	acceptor_gain	1.0000
19:6213408:CC:C	acceptor_gain	1.0000
19:6213409:C:CC	acceptor_gain	1.0000
19:6213409:C:T	acceptor_gain	1.0000
19:6213410:T:A	acceptor_loss	1.0000
19:6213723:CACC:C	donor_loss	1.0000
19:6213724:AC:A	donor_loss	1.0000
19:6213725:CCTTG:C	donor_loss	1.0000
19:6213795:CAC:C	acceptor_gain	1.0000
19:6213796:ACCTG:A	acceptor_loss	1.0000
19:6213797:CCTG:C	acceptor_loss	1.0000
19:6213798:C:CC	acceptor_gain	1.0000
19:6213934:CTCAC:C	donor_loss	1.0000
19:6213937:A:AT	donor_loss	1.0000
19:6213938:C:CG	donor_loss	1.0000
19:6213938:CCTTG:C	donor_gain	1.0000
19:6213982:CGG:C	donor_gain	1.0000
19:6214034:TCAAC:T	acceptor_gain	1.0000

AlphaMissense

3686 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:6213073:A:G	L550P	1.000
19:6213097:A:G	L542P	1.000
19:6213106:A:G	L539P	1.000
19:6213106:A:T	L539H	1.000
19:6213111:G:C	F537L	1.000
19:6213111:G:T	F537L	1.000
19:6213112:A:G	F537S	1.000
19:6213113:A:G	F537L	1.000
19:6213118:A:G	F535S	1.000
19:6213138:G:C	F528L	1.000
19:6213138:G:T	F528L	1.000
19:6213140:A:G	F528L	1.000
19:6213157:A:T	I522N	1.000
19:6213160:A:G	L521P	1.000
19:6213371:A:G	L506P	1.000
19:6213381:G:C	H503D	1.000
19:6213383:A:G	L502P	1.000
19:6213392:A:G	L499P	1.000
19:6230571:C:T	G140E	1.000
19:6230586:A:G	L135P	1.000
19:6230586:A:T	L135H	1.000
19:6230598:A:G	F131S	1.000
19:6230610:G:T	P127H	1.000
19:6230618:G:C	F124L	1.000
19:6230618:G:T	F124L	1.000
19:6230619:A:G	F124S	1.000
19:6230620:A:G	F124L	1.000
19:6230625:A:G	L122P	1.000
19:6230673:A:G	L106P	1.000
19:6230673:A:T	L106Q	1.000

dbSNP variants (sampled 300 via entrez): RS1000040978 (19:6228172 G>A), RS1000046459 (19:6261392 G>T), RS1000072322 (19:6267127 A>T), RS1000178917 (19:6240711 C>T), RS1000181700 (19:6252458 G>GA), RS1000197529 (19:6276177 T>C), RS1000212101 (19:6211357 C>A,T), RS1000264717 (19:6218964 T>C), RS1000316106 (19:6215100 G>A), RS1000321270 (19:6215309 T>A,C), RS1000331963 (19:6237294 TC>T), RS1000345891 (19:6214971 G>A), RS1000346290 (19:6211570 G>A), RS1000382719 (19:6256683 G>A), RS1000416381 (19:6276900 A>C)

Disease associations

OMIM: gene MIM:159556 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST003472_2	Oppositional defiant disorder dimensions in attention-deficit hyperactivity disorder	5.000000e-06
GCST90002393_636	Monocyte count	1.000000e-15
GCST90002394_435	Monocyte percentage of white cells	2.000000e-13

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0007679	oppositional defiant disorder measurement
EFO:0005091	monocyte count
EFO:0007989	monocyte percentage of leukocytes

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4295801 (SINGLE PROTEIN), CHEMBL6066148 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,538 (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
CHEMBL1232461	MOLIBRESIB	2	1,538

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — Acylated lysine reader proteins

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

Ligand	Action	Affinity	Parameter
SR-0813	Inhibition	7.52	pKd

Binding affinities (BindingDB)

105 measured of 105 human assays (105 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
1-amino-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]isoquinoline-6-carboxamide	IC50	14 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-(difluoromethyl)-1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-6-carboxamide	IC50	14 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-(methylamino)-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]isoquinoline-6-carboxamide	IC50	15 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
2-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]pyrazolo[1,5-a]pyridine-6-carboxamide	IC50	17 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-fluoro-1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-6-carboxamide	IC50	18 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]isoquinoline-6-carboxamide	IC50	18 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]isoquinoline-6-carboxamide	IC50	18 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-cyclopropyl-1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-6-carboxamide	IC50	21 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methoxy-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]isoquinoline-6-carboxamide	IC50	25 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-5-carboxamide	IC50	26 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methoxy-4-(methylamino)-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]quinoline-7-carboxamide	IC50	28 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
2-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]quinoline-6-carboxamide	IC50	29 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-2-oxo-3H-benzimidazole-5-carboxamide	IC50	30 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-1-pyridin-4-ylindazole-5-carboxamide	IC50	31 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1,3-dimethyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-6-carboxamide	IC50	34 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-cyclopropyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]imidazo[1,5-a]pyridine-7-carboxamide	IC50	35 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-chloro-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-2H-indazole-5-carboxamide	IC50	37 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1,3-dimethyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]imidazo[1,5-a]pyridine-6-carboxamide	IC50	38 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1,3-dimethyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-2H-benzotriazole-5-carboxamide	IC50	41 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-2H-indazole-5-carboxamide	IC50	42 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]pyrazolo[1,5-a]pyridine-5-carboxamide	IC50	43 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1,3-dimethyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-6-carboxamide	IC50	43 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1,3-dimethyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-5-carboxamide	IC50	47 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]isoquinoline-7-carboxamide	IC50	47 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]pyrazolo[1,5-a]pyridine-6-carboxamide	IC50	48 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-1,2-benzoxazole-6-carboxamide	IC50	51 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-fluoro-1-methyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-6-carboxamide	IC50	51 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1,3-dimethyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]imidazo[1,5-a]pyridine-6-carboxamide	IC50	51 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
7-fluoro-2-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-3H-benzimidazol-5-yl]quinoline-6-carboxamide	IC50	53 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]benzimidazole-5-carboxamide	IC50	53 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]imidazo[1,5-a]pyridine-6-carboxamide	IC50	55 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1,3-dimethyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]imidazo[1,5-a]pyridine-6-carboxamide	IC50	56 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-1-pyridin-4-ylbenzotriazole-5-carboxamide	IC50	56 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-2-oxoquinoline-6-carboxamide	IC50	56 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-2H-indazole-5-carboxamide	IC50	57 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]imidazo[1,5-a]pyridine-6-carboxamide	IC50	58 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-5-carboxamide	IC50	58 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-chloro-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-2H-indazole-5-carboxamide	IC50	61 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]isoquinoline-7-carboxamide	IC50	64 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-3-propan-2-ylimidazo[1,5-a]pyridine-7-carboxamide	IC50	75 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1,4-dimethyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]phthalazine-6-carboxamide	IC50	76 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-2-oxopyrazolo[1,5-a]pyridine-6-carboxamide	IC50	76 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methyl-N-[2-(1-methylpyrrolidin-2-yl)-3H-benzimidazol-5-yl]-1,2-benzoxazole-6-carboxamide	IC50	78 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
7-fluoro-2-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-b]pyridin-6-yl]quinoline-6-carboxamide	IC50	78 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3,7-difluoro-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-b]pyridin-6-yl]-2H-indazole-6-carboxamide	IC50	79 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]imidazo[1,5-a]pyridine-7-carboxamide	IC50	84 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
7-fluoro-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-3H-benzimidazol-5-yl]quinoline-6-carboxamide	IC50	88 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
2-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]-3H-benzimidazole-5-carboxamide	IC50	90 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
3-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]triazolo[1,5-a]pyridine-6-carboxamide	IC50	91 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS
1-methyl-N-[2-[(2R)-1-methylpiperidin-2-yl]-1H-pyrrolo[3,2-c]pyridin-6-yl]imidazo[1,5-a]pyridine-7-carboxamide	IC50	93 nM	US-20250136592: C-LINKED INHIBITORS OF ENL/AF9 YEATS

ChEMBL bioactivities

208 potent at pChembl≥5 of 235 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.85	Ki	1.43	nM	CHEMBL4210431
8.70	Kd	2	nM	CHEMBL6151956
8.47	Ki	3.37	nM	CHEMBL5187921
7.97	IC50	10.7	nM	CHEMBL5400413
7.85	IC50	14	nM	CHEMBL4552313
7.84	IC50	14.5	nM	CHEMBL5423431
7.81	IC50	15.4	nM	CHEMBL5438748
7.77	IC50	17	nM	CHEMBL5397340
7.77	Kd	17	nM	CHEMBL5438748
7.76	IC50	17.2	nM	CHEMBL5411777
7.75	IC50	17.9	nM	CHEMBL4552313
7.72	IC50	18.9	nM	CHEMBL5404010
7.72	IC50	19.2	nM	CHEMBL5427068
7.66	IC50	22	nM	CHEMBL5416453
7.66	IC50	22.1	nM	CHEMBL5430847
7.61	Kd	24.5	nM	CHEMBL4552313
7.60	IC50	25	nM	CHEMBL5418436
7.55	IC50	28.2	nM	CHEMBL5400474
7.52	Kd	30	nM	CHEMBL5418436
7.50	IC50	31.8	nM	CHEMBL5421344
7.49	IC50	32.3	nM	CHEMBL5414763
7.45	IC50	35.3	nM	CHEMBL5395585
7.45	IC50	35.4	nM	CHEMBL5438461
7.44	Kd	36.3	nM	CHEMBL6132727
7.43	IC50	36.7	nM	CHEMBL5429534
7.42	IC50	37.9	nM	CHEMBL5417838
7.40	IC50	40	nM	CHEMBL5437942
7.40	IC50	40	nM	CHEMBL6143618
7.35	Kd	45	nM	CHEMBL4863719
7.34	Kd	46	nM	CHEMBL4865432
7.34	IC50	46	nM	CHEMBL5428707
7.33	IC50	46.4	nM	CHEMBL5406254
7.31	IC50	48.8	nM	CHEMBL5404615
7.30	IC50	50	nM	CHEMBL5395794
7.29	IC50	51	nM	CHEMBL4863719
7.25	Ki	56	nM	CHEMBL4211714
7.25	IC50	56.4	nM	CHEMBL5403698
7.24	Kd	57	nM	CHEMBL4204744
7.20	Ki	63	nM	CHEMBL4204744
7.15	IC50	70.2	nM	CHEMBL5419393
7.14	IC50	72.2	nM	CHEMBL5420860
7.12	Kd	75	nM	CHEMBL4800073
7.11	IC50	77	nM	CHEMBL5416650
7.09	Kd	82	nM	CHEMBL4752253
7.07	IC50	85	nM	CHEMBL4865432
7.05	Ki	90	nM	CHEMBL4216416
7.05	Kd	90	nM	MOLIBRESIB
7.05	Kd	89	nM	MOLIBRESIB
7.00	Ki	101	nM	CHEMBL4211204
7.00	Kd	100	nM	CHEMBL4552313

PubChem BioAssay actives

175 with measured affinity, of 390 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)-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	1911457: Binding affinity to MBP-tagged human recombinant ENL (489 to 559 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0014	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	1911457: Binding affinity to MBP-tagged human recombinant ENL (489 to 559 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.0034	uM
3-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-1,2-benzoxazole-6-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0107	uM
1-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0140	uM
N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-1-(2-morpholin-4-ylethyl)indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0145	uM
5-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-6-oxophenanthridine-2-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0154	uM
1-butyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0170	uM
2-(2-aminoethyl)-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0172	uM
1-ethyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0189	uM
1-(2-benzamidoethyl)-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0192	uM
3,4-dihydroxy-2,5-bis(hydroxymethyl)-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]pyrrolidine-1-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0220	uM
9-fluoro-5-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-6-oxophenanthridine-2-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0221	uM
N-cyclobutyl-2-[3-(2-piperidin-1-ylethylsulfamoylamino)phenyl]imidazo[1,2-a]pyridine-6-carboxamide	1969446: Inhibition of recombinant C-terminal 6-His tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21 cells using H3K27cr as substrate incubated for 2 hrs by HTRF assay	ic50	0.0250	uM
1-(2-aminoethyl)-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0282	uM
5-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-6-oxophenanthridine-3-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0318	uM
1-[2-[2-(1,2-dihydroxyethyl)-3,4-dihydroxypyrrolidin-1-yl]ethyl]-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0323	uM
2-butyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0353	uM
1-[2-[(2-methylbenzoyl)amino]ethyl]-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0354	uM
2-ethyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0367	uM
tert-butyl N-[2-[5-[[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]carbamoyl]indazol-2-yl]ethyl]carbamate	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0379	uM
1-methyl-N-[2-[(2R)-1-methylpyrrolidin-2-yl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1993774: Inhibition of 5x6His-tagged ENL YEATS domain (unknown origin) using biotinylated peptide H3K9cr (1 to 20 residues) preincubated for 15 mins followed by substrate addition and measured after 30 mins by TR-FRET assay	ic50	0.0400	uM
N-[[4-(azetidin-1-ylmethyl)phenyl]methyl]-[1,2,4]triazolo[4,3-a]pyridine-6-carboxamide	1751795: Binding affinity to human His-ENL YEATS domain assessed as dissociation constant by SPR analysis	kd	0.0450	uM
N-[[4-[[(5-fluoropyrimidin-2-yl)amino]methyl]phenyl]methyl]-[1,2,4]triazolo[4,3-a]pyridine-6-carboxamide	1751795: Binding affinity to human His-ENL YEATS domain assessed as dissociation constant by SPR analysis	kd	0.0460	uM
1-[2-[(3-fluorophenyl)carbamoylamino]ethyl]-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0460	uM
5,10-dimethyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-6-oxophenanthridine-2-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0464	uM
3-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-1,2-benzoxazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0488	uM
1-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-1H-pyrrolo[3,2-c]pyridin-6-yl]indazole-5-carboxamide	1969440: Inhibition of 3xFLAG-HA-tagged wild-type human ENL YEATS domain using biotinylated peptide as substrate preincubated for 15 mins followed by substrate addition and incubated for 30 mins by TR-FRET Assay	ic50	0.0500	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	1387577: Displacement of N-Flu-DOT1L from MBP-tagged ENL (unknown origin) (489 to 559 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0560	uM
1-[2-[4-(2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyl-3a,4,6,6a-tetrahydro-[1,3]dioxolo[4,5-c]pyrrol-5-yl]ethyl]-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0564	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	1387579: Binding affinity to MBP-tagged ENL (unknown origin) (489 to 559 residues) expressed in Escherichia coli BL21(DE3) by Bio-layer interferometry	kd	0.0570	uM
2-cyclopentyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0702	uM
9-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]carbazole-2-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0722	uM
2-methyl-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]indazole-5-carboxamide	1969422: Inhibition of C-terminal 6xHis-tagged ENL YEATS domain (1 to 148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using biotin-H3K27ace as substrate incubated for 45 mins by alpha screen assay	ic50	0.0770	uM
N-[(1R)-2,3-dihydro-1H-inden-1-yl]-5-[4-(dimethylcarbamoyl)-3-hydroxyphenyl]-1,2-oxazole-3-carboxamide	2004074: Binding affinity to MLLT1 YD domain (unknown origin) assessed as dissociation constant by isothermal calorimetry assay	kd	0.0820	uM
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide	2179106: Binding affinity against MLLT1 (unknown origin) assessed as apparent dissociation constant incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	kd	0.0890	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	1387577: Displacement of N-Flu-DOT1L from MBP-tagged ENL (unknown origin) (489 to 559 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.0900	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	1387577: Displacement of N-Flu-DOT1L from MBP-tagged ENL (unknown origin) (489 to 559 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.1010	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	1911457: Binding affinity to MBP-tagged human recombinant ENL (489 to 559 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.1090	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	1911457: Binding affinity to MBP-tagged human recombinant ENL (489 to 559 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.1120	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-benzoylpyrrolidine-2-carboxamide	1387577: Displacement of N-Flu-DOT1L from MBP-tagged ENL (unknown origin) (489 to 559 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.1190	uM
N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-4-pyrazin-2-ylbenzamide	1993774: Inhibition of 5x6His-tagged ENL YEATS domain (unknown origin) using biotinylated peptide H3K9cr (1 to 20 residues) preincubated for 15 mins followed by substrate addition and measured after 30 mins by TR-FRET assay	ic50	0.1300	uM
2-fluoro-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-1H-pyrrolo[3,2-b]pyridin-6-yl]-4-pyrazin-2-ylbenzamide	1993774: Inhibition of 5x6His-tagged ENL YEATS domain (unknown origin) using biotinylated peptide H3K9cr (1 to 20 residues) preincubated for 15 mins followed by substrate addition and measured after 30 mins by TR-FRET assay	ic50	0.1300	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	1387577: Displacement of N-Flu-DOT1L from MBP-tagged ENL (unknown origin) (489 to 559 residues) expressed in Escherichia coli BL21(DE3) measured after 3 hrs by fluorescence polarization assay	ki	0.1500	uM
4-chloro-2-fluoro-N-[6-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-5H-pyrrolo[3,2-c]pyridazin-3-yl]benzamide	1993774: Inhibition of 5x6His-tagged ENL YEATS domain (unknown origin) using biotinylated peptide H3K9cr (1 to 20 residues) preincubated for 15 mins followed by substrate addition and measured after 30 mins by TR-FRET assay	ic50	0.1500	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	1911457: Binding affinity to MBP-tagged human recombinant ENL (489 to 559 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.1570	uM
2-fluoro-N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-4-pyrazin-2-ylbenzamide	1993778: Binding affinity to ENL YEATS domain (unknown origin) at 100 uM by ITC analysis	kd	0.1600	uM
N-cyclopentyl-5-[4-(dimethylcarbamoyl)-3-hydroxyphenyl]-1,2-oxazole-3-carboxamide	2004066: Inhibition of MLLT1 YD domain (unknown origin) assessed as disruption of histone peptide binding using histone peptide as substrate by HTRF assay	ic50	0.1600	uM
2-fluoro-N-[6-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-5H-pyrrolo[3,2-c]pyridazin-3-yl]-4-pyrazin-2-ylbenzamide	1993774: Inhibition of 5x6His-tagged ENL YEATS domain (unknown origin) using biotinylated peptide H3K9cr (1 to 20 residues) preincubated for 15 mins followed by substrate addition and measured after 30 mins by TR-FRET assay	ic50	0.1700	uM
N-[2-[[(2S)-2-methylpyrrolidin-1-yl]methyl]-3H-benzimidazol-5-yl]-4-pyrimidin-4-ylbenzamide	1993774: Inhibition of 5x6His-tagged ENL YEATS domain (unknown origin) using biotinylated peptide H3K9cr (1 to 20 residues) preincubated for 15 mins followed by substrate addition and measured after 30 mins by TR-FRET assay	ic50	0.1800	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	1911457: Binding affinity to MBP-tagged human recombinant ENL (489 to 559 residues) incubated for 40 mins by measuring fluorescence polarization by microplate reader method	ki	0.1840	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, affects cotreatment, increases abundance, increases expression	3
Arsenic	affects cotreatment, increases abundance, increases expression, affects methylation	2
FR900359	increases phosphorylation	1
TAK-243	increases sumoylation	1
dicrotophos	increases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	increases expression	1
lead acetate	increases expression	1
butyraldehyde	decreases expression	1
manganese chloride	affects cotreatment, increases abundance, increases expression	1
aflatoxin B2	decreases methylation	1
coumarin	increases phosphorylation	1
phenanthrene	decreases expression	1
perfluoro-n-nonanoic acid	decreases expression	1
bisphenol S	affects cotreatment, increases methylation	1
Resveratrol	affects cotreatment, decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Air Pollutants	increases abundance, increases expression	1
Atrazine	increases expression	1
Cisplatin	decreases expression	1
Dimethyl Sulfoxide	increases expression	1
Doxorubicin	decreases expression	1
Endosulfan	affects cotreatment, increases expression	1
Manganese	affects cotreatment, increases abundance, increases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Ribonucleotides	affects binding	1
Rotenone	decreases expression	1
Smoke	decreases expression	1
Tetrachlorodibenzodioxin	affects cotreatment, increases expression	1
Aflatoxin B1	decreases methylation	1

ChEMBL screening assays

95 unique, capped per target: 94 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4202267	Binding	Displacement of N-Flu-DOT1L from MBP-tagged ENL (unknown origin) (489 to 559 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
CHEMBL5723286	Functional	Affinity Biochemical interaction: (Homogeneous TR-FRET) EUB0002726a MLLT1	Affinity Biochemical Literature for EUbOPEN Chemogenomic Library

Cellosaurus cell lines

13 cell lines: 6 cancer cell line, 4 transformed cell line, 3 embryonic stem cell

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

Cellosaurus	Name	Category	Sex
CVCL_1866	KOPN-8	Cancer cell line	Female
CVCL_3937	KOPN-1	Cancer cell line	Female
CVCL_3991	KOCL-33	Cancer cell line	Female
CVCL_6865	KOCL-51	Cancer cell line	Male
CVCL_8227	HB11;19	Cancer cell line	Sex unspecified
CVCL_8485	Kasumi-10	Cancer cell line	Female
CVCL_A4E3	SEES3-1V human MLLT1, clone1	Embryonic stem cell	Male
CVCL_A4E4	SEES3-1V human MLLT1, clone2	Embryonic stem cell	Male
CVCL_A4E5	SEES3-1V human MLLT1, clone3	Embryonic stem cell	Male
CVCL_A8IE	M9-ENL1	Transformed cell line

Clinical trials (associated diseases)

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