MON2

Summary

MON2 (MON2 regulator of endosome-to-Golgi trafficking, HGNC:29177) is a protein-coding gene on chromosome 12q14.1, encoding Protein MON2 homolog (Q7Z3U7). Plays a role in regulating membrane trafficking of cargo proteins. It is a selective cancer dependency (DepMap: 11.8% of cell lines).

Predicted to enable proton transmembrane transporter activity. Predicted to be involved in Golgi to endosome transport. Located in early endosome membrane.

Source: NCBI Gene 23041 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 197 total
• Druggable target: yes
• Cancer dependency (DepMap): dependent in 11.8% of screened cell lines
• MANE Select transcript: NM_015026

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:29177
Approved symbol	MON2
Name	MON2 regulator of endosome-to-Golgi trafficking
Location	12q14.1
Locus type	gene with protein product
Status	Approved
Aliases	KIAA1040
Ensembl gene	ENSG00000061987
Ensembl biotype	protein_coding
OMIM	616822
Entrez	23041

Gene structure

Transcript identifiers

Ensembl transcripts: 21 — 13 protein_coding, 5 retained_intron, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000393629, ENST00000393630, ENST00000546600, ENST00000546751, ENST00000547095, ENST00000547287, ENST00000549286, ENST00000549378, ENST00000549539, ENST00000551307, ENST00000551397, ENST00000552115, ENST00000552738, ENST00000641654, ENST00000854041, ENST00000854042, ENST00000854043, ENST00000914365, ENST00000953601, ENST00000953602, ENST00000953603

RefSeq mRNA: 5 — MANE Select: NM_015026 NM_001278469, NM_001278470, NM_001278471, NM_001278472, NM_015026

CCDS: CCDS31849, CCDS61175, CCDS61177, CCDS61178

Canonical transcript exons

ENST00000393630 — 35 exons

Exon	Start	End
ENSE00001358622	62592586	62600476
ENSE00003459455	62532438	62532670
ENSE00003464043	62508286	62508480
ENSE00003468543	62580297	62580420
ENSE00003470669	62535525	62535709
ENSE00003472122	62566014	62566031
ENSE00003486231	62588074	62588156
ENSE00003490119	62538096	62538176
ENSE00003497690	62493915	62494042
ENSE00003501225	62565237	62565380
ENSE00003507393	62560491	62561113
ENSE00003514713	62537151	62537263
ENSE00003515746	62585294	62585501
ENSE00003516432	62555994	62556192
ENSE00003525510	62544898	62545008
ENSE00003547960	62571392	62571582
ENSE00003552003	62534845	62534926
ENSE00003559463	62525949	62526102
ENSE00003566789	62538415	62538505
ENSE00003576516	62552881	62553174
ENSE00003578128	62546897	62547072
ENSE00003578227	62578445	62578505
ENSE00003578575	62501573	62501698
ENSE00003578903	62537602	62537706
ENSE00003579576	62484170	62484233
ENSE00003583757	62543097	62543198
ENSE00003584395	62524515	62524639
ENSE00003606969	62498919	62499048
ENSE00003637152	62495016	62495147
ENSE00003639645	62538252	62538325
ENSE00003647058	62566322	62566450
ENSE00003656431	62525084	62525220
ENSE00003670276	62500783	62500880
ENSE00003690110	62549668	62549830
ENSE00003841246	62466826	62467318

Expression profiles

Bgee: expression breadth ubiquitous, 289 present calls, max score 95.98.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 32.6418 / max 342.1206, expressed in 1815 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
126396	32.6418	1815

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
body of pancreas	UBERON:0001150	95.98	gold quality
tibia	UBERON:0000979	95.44	gold quality
calcaneal tendon	UBERON:0003701	94.80	gold quality
mucosa of paranasal sinus	UBERON:0005030	94.71	gold quality
tibial nerve	UBERON:0001323	94.61	gold quality
adrenal tissue	UBERON:0018303	94.54	gold quality
corpus callosum	UBERON:0002336	94.38	gold quality
right uterine tube	UBERON:0001302	94.20	gold quality
skin of leg	UBERON:0001511	93.51	gold quality
left ovary	UBERON:0002119	93.45	gold quality
skin of abdomen	UBERON:0001416	93.34	gold quality
minor salivary gland	UBERON:0001830	93.33	gold quality
pylorus	UBERON:0001166	93.24	gold quality
mucosa of stomach	UBERON:0001199	93.22	gold quality
left lobe of thyroid gland	UBERON:0001120	93.07	gold quality
adenohypophysis	UBERON:0002196	92.98	gold quality
right lobe of liver	UBERON:0001114	92.97	gold quality
endocervix	UBERON:0000458	92.96	gold quality
descending thoracic aorta	UBERON:0002345	92.93	gold quality
right ovary	UBERON:0002118	92.90	gold quality
superficial temporal artery	UBERON:0001614	92.89	gold quality
thyroid gland	UBERON:0002046	92.89	gold quality
right lobe of thyroid gland	UBERON:0001119	92.75	gold quality
superior surface of tongue	UBERON:0007371	92.72	gold quality
saliva-secreting gland	UBERON:0001044	92.70	gold quality
zone of skin	UBERON:0000014	92.61	gold quality
pituitary gland	UBERON:0000007	92.60	gold quality
popliteal artery	UBERON:0002250	92.59	gold quality
tibial artery	UBERON:0007610	92.59	gold quality
aorta	UBERON:0000947	92.49	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	6.09

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

227 targeting MON2, 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-3163	100.00	77.23	8605
HSA-MIR-5692A	100.00	74.40	6850
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-200B-3P	100.00	73.31	2693
HSA-MIR-200C-3P	100.00	73.35	2685
HSA-MIR-429	100.00	73.44	2698
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-LET-7F-2-3P	99.98	70.98	2588
HSA-MIR-1185-1-3P	99.98	71.04	2593
HSA-MIR-1185-2-3P	99.98	71.04	2593
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 11.8% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 5)

• Ysl2p represents an essential, evolutionarily conserved member of a network controlling direct binding and membrane docking of Ggas. (PMID:18418388)
• Depletion of hVps18 or hMon2 reduced the efficient production of infectious HIV-1 virions in human cells. (PMID:21450827)
• Mon2 is involved in endosome-to-Golgi trafficking as its depletion accelerated the delivery of furin and CI-M6PR to Golgi after endocytosis. (PMID:24285343)
• an evolutionary conserved MON2:DOPEY2:ATP9A complex is required for SNX3 retromer mediation of Wntless sorting and Wnt secretion (PMID:30213940)
• MicroRNA-133a-5p inhibiting metastatic capacity of renal clear cell carcinoma through regulating MON2. (PMID:32572912)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	mon2	ENSDARG00000099798
mus_musculus	Mon2	ENSMUSG00000034602
rattus_norvegicus	Mon2	ENSRNOG00000004185
drosophila_melanogaster	mon2	FBGN0031985
caenorhabditis_elegans		WBGENE00008685

Paralogs (15): CYTH3 (ENSG00000008256), PSD (ENSG00000059915), ARFGEF1 (ENSG00000066777), CYTH4 (ENSG00000100055), CYTH2 (ENSG00000105443), GBF1 (ENSG00000107862), CYTH1 (ENSG00000108669), IQSEC3 (ENSG00000120645), ARFGEF2 (ENSG00000124198), IQSEC2 (ENSG00000124313), PSD4 (ENSG00000125637), IQSEC1 (ENSG00000144711), PSD2 (ENSG00000146005), PSD3 (ENSG00000156011), FBXO8 (ENSG00000164117)

Protein

Protein identifiers

Protein MON2 homolog — Q7Z3U7 (reviewed: Q7Z3U7)

Alternative names: Protein SF21

All UniProt accessions (5): Q7Z3U7, A0A286YFF8, F8VQS2, F8VZV1, F8VZV6

UniProt curated annotations — full annotation on UniProt →

Function. Plays a role in regulating membrane trafficking of cargo proteins. Together with ATP9A and DOP1B, regulates SNX3 retromer-mediated endosomal sorting of WLS away from lysosomal degradation.

Subunit / interactions. Homooligomer. Heterotrimer with ATP9A and DOP1B; this interaction is retromer-independent. Interacts with SNX3.

Subcellular location. Early endosome membrane.

Similarity. Belongs to the MON2 family.

Isoforms (5)

UniProt ID	Names	Canonical?
Q7Z3U7-1	1	yes
Q7Z3U7-2	2
Q7Z3U7-3	3
Q7Z3U7-5	5
Q7Z3U7-6	6

RefSeq proteins (5): NP_001265398, NP_001265399, NP_001265400, NP_001265401, NP_055841* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR015403	Mon2/Sec7/BIG1-like_HDS	Domain
IPR016024	ARM-type_fold	Homologous_superfamily
IPR032629	DCB_dom	Domain
IPR032691	Mon2/Sec7/BIG1-like_HUS	Domain
IPR032817	Mon2_C	Domain

Pfam: PF09324, PF12783, PF16206, PF16213

UniProt features (22 total): sequence conflict 8, splice variant 6, modified residue 3, initiator methionine 1, chain 1, sequence variant 1, region of interest 1, compositionally biased region 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q7Z3U7-F1	78.50	0.30

Functional residue map

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

Post-translational modifications (3): 2, 205, 537

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 207 (showing top): GSE45365_NK_CELL_VS_CD8A_DC_UP, GSE45365_NK_CELL_VS_BCELL_UP, MORF_FLT1, YAGI_AML_WITH_INV_16_TRANSLOCATION, MORF_MSH3, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, GOBP_PROTEIN_TARGETING, GOBP_VACUOLAR_TRANSPORT, GOBP_VESICLE_MEDIATED_TRANSPORT, GOBP_ESTABLISHMENT_OF_PROTEIN_LOCALIZATION_TO_ORGANELLE, MORF_RAD51L3, GOBP_REGULATION_OF_VESICLE_MEDIATED_TRANSPORT, GOBP_PROTEIN_LOCALIZATION_TO_VACUOLE, GOBP_REGULATION_OF_CELLULAR_LOCALIZATION, ACATTCC_MIR1_MIR206

GO Biological Process (2): Golgi to endosome transport (GO:0006895), protein transport (GO:0015031)

GO Molecular Function (2): guanyl-nucleotide exchange factor activity (GO:0005085), protein binding (GO:0005515)

GO Cellular Component (5): cytosol (GO:0005829), early endosome membrane (GO:0031901), extracellular exosome (GO:0070062), endosome (GO:0005768), membrane (GO:0016020)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	2
post-Golgi vesicle-mediated transport	1
intercellular transport	1
cytosolic transport	1
transport	1
intracellular protein localization	1
establishment of protein localization	1
GTP binding	1
GDP binding	1
GTPase regulator activity	1
binding	1
cytoplasm	1
early endosome	1
endosome membrane	1
extracellular vesicle	1
endomembrane system	1
cytoplasmic vesicle	1

Protein interactions and networks

STRING

1590 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MON2	DOP1A	Q5JWR5	877
MON2	DOP1B	Q9Y3R5	590
MON2	FBXO38	Q6PIJ6	559
MON2	SNX3	O60493	536
MON2	ATP9A	O75110	513
MON2	ATP9B	O43861	506
MON2	TBC1D22A	Q8WUA7	503
MON2	CDC40	O60508	489
MON2	FCGR3A	P08637	479
MON2	FCGR3B	O75015	479
MON2	VPS29	Q9UBQ0	476
MON2	ARL3	P36405	475
MON2	AP3D1	O14617	471
MON2	ARFRP1	Q13795	466
MON2	RIC1	Q4ADV7	458

IntAct

146 interactions, top by confidence:

A	B	Type	Score
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
SPTLC1	SPTLC2	psi-mi:“MI:0914”(association)	0.680
DOP1A	MON2	psi-mi:“MI:0915”(physical association)	0.680
MON2	DOP1A	psi-mi:“MI:0915”(physical association)	0.680
MON2	DOP1A	psi-mi:“MI:0407”(direct interaction)	0.680
DOP1A	MON2	psi-mi:“MI:0403”(colocalization)	0.680
DOP1A	MON2	psi-mi:“MI:0914”(association)	0.680
SDC2	PDPK1	psi-mi:“MI:0914”(association)	0.640
KLC2	DOP1A	psi-mi:“MI:0914”(association)	0.590
MON2	MON2	psi-mi:“MI:0915”(physical association)	0.540
MON2	MON2	psi-mi:“MI:0407”(direct interaction)	0.540
	DOP1A	psi-mi:“MI:0915”(physical association)	0.540
EGFR	NDUFA4	psi-mi:“MI:0914”(association)	0.530
ARRDC4	WWP2	psi-mi:“MI:0914”(association)	0.530
NPY2R	RTL8C	psi-mi:“MI:0914”(association)	0.530
VASN	AP3B1	psi-mi:“MI:0914”(association)	0.530
CA14	EXOC5	psi-mi:“MI:0914”(association)	0.530
TMEM9	ESYT2	psi-mi:“MI:0914”(association)	0.530
TNFSF8	LGALS8	psi-mi:“MI:0914”(association)	0.530
CD40	EXOC5	psi-mi:“MI:0914”(association)	0.530
GGA1	MON2	psi-mi:“MI:0915”(physical association)	0.520
MON2	GGA1	psi-mi:“MI:0915”(physical association)	0.520
STOM	EI24	psi-mi:“MI:0914”(association)	0.510

BioGRID (194): MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS), STOM (Affinity Capture-MS), MON2 (Two-hybrid), MON2 (Affinity Capture-MS), MON2 (Affinity Capture-MS)

ESM2 similar proteins: A0A0R4ITC5, A1L1F4, A4L9P7, E9Q8I9, F1MKX4, F1QFR9, F1R2X6, F8VPU6, O94915, P21359, P42345, P42346, P51593, P97526, Q04690, Q14997, Q29RF7, Q2HJG5, Q498H0, Q4KLU7, Q4QXM3, Q4VA53, Q5F3U9, Q5F3V3, Q5R6J0, Q5SSW2, Q5TBA9, Q5U241, Q5VYK3, Q6A026, Q6DDM4, Q6GP04, Q6NRP2, Q6P4S8, Q6PDI5, Q6TRW4, Q7PX35, Q7TMY8, Q7Z3U7, Q7Z6Z7

Diamond homologs: Q19338, Q29L43, Q61SD1, Q6GP04, Q7Z3U7, Q80TL7, Q9VLT1

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
MON2	“form complex”	“ATP9A-DOP1B-MON2, golgi transporter complex”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 168 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
TNFs bind their physiological receptors	5	19.3×	3e-03

GO biological processes:

GO term	Partners	Fold	FDR
peptidyl-tyrosine phosphorylation	6	18.1×	5e-04
T cell costimulation	5	13.4×	8e-03
protein autophosphorylation	8	8.3×	2e-03
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	12	6.7×	3e-04
positive regulation of MAPK cascade	10	5.8×	3e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	154
Likely benign	5
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

6157 predictions. Top by Δscore:

Variant	Effect	Δscore
12:62467316:GAG:G	donor_gain	1.0000
12:62467318:GGTAA:G	donor_loss	1.0000
12:62467319:G:T	donor_loss	1.0000
12:62467320:T:G	donor_loss	1.0000
12:62470776:GTT:G	donor_gain	1.0000
12:62487078:A:AG	acceptor_gain	1.0000
12:62487078:ACT:A	acceptor_gain	1.0000
12:62487080:T:A	acceptor_gain	1.0000
12:62493898:A:AG	acceptor_gain	1.0000
12:62493898:AT:A	acceptor_gain	1.0000
12:62493899:T:G	acceptor_gain	1.0000
12:62493907:A:AG	acceptor_gain	1.0000
12:62493908:A:G	acceptor_gain	1.0000
12:62493910:T:G	acceptor_gain	1.0000
12:62498914:TTCA:T	acceptor_loss	1.0000
12:62498915:TCA:T	acceptor_loss	1.0000
12:62498917:A:AG	acceptor_gain	1.0000
12:62498917:A:AT	acceptor_loss	1.0000
12:62498917:AG:A	acceptor_gain	1.0000
12:62498918:G:GG	acceptor_gain	1.0000
12:62498918:GG:G	acceptor_gain	1.0000
12:62498918:GGC:G	acceptor_gain	1.0000
12:62498918:GGCA:G	acceptor_gain	1.0000
12:62499046:GAG:G	donor_gain	1.0000
12:62499047:AGGTA:A	donor_loss	1.0000
12:62499049:G:C	donor_loss	1.0000
12:62499049:G:GG	donor_gain	1.0000
12:62501699:G:GG	donor_gain	1.0000
12:62508280:A:AG	acceptor_gain	1.0000
12:62508281:A:G	acceptor_gain	1.0000

AlphaMissense

11193 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:62467311:T:A	V35D	1.000
12:62484170:G:C	A38P	1.000
12:62484173:G:C	A39P	1.000
12:62484174:C:A	A39D	1.000
12:62493948:C:G	P70R	1.000
12:62493959:G:C	G74R	1.000
12:62493960:G:A	G74D	1.000
12:62493962:T:C	C75R	1.000
12:62493995:T:C	C86R	1.000
12:62493997:T:G	C86W	1.000
12:62494017:T:C	L93P	1.000
12:62495044:T:C	L111P	1.000
12:62495053:T:C	L114P	1.000
12:62495077:T:A	L122H	1.000
12:62495083:T:C	L124P	1.000
12:62495086:T:A	L125H	1.000
12:62495086:T:C	L125P	1.000
12:62498926:T:A	V148D	1.000
12:62498929:T:C	L149P	1.000
12:62498931:T:C	C150R	1.000
12:62498932:G:A	C150Y	1.000
12:62498933:T:G	C150W	1.000
12:62498938:G:C	R152P	1.000
12:62498941:T:C	L153P	1.000
12:62498946:T:C	F155L	1.000
12:62498948:C:A	F155L	1.000
12:62498948:C:G	F155L	1.000
12:62498976:G:C	A165P	1.000
12:62498977:C:A	A165D	1.000
12:62498982:G:C	A167P	1.000

dbSNP variants (sampled 300 via entrez): RS1000014020 (12:62584521 G>A), RS1000035362 (12:62478440 T>C), RS1000056895 (12:62578336 A>C,G), RS1000115433 (12:62522698 T>C), RS1000149349 (12:62584796 G>A), RS1000168149 (12:62521759 T>G), RS1000171778 (12:62557666 T>G), RS1000193913 (12:62510283 T>C), RS1000209990 (12:62516865 C>T), RS1000221118 (12:62558440 C>A,T), RS1000248675 (12:62505106 GTGT>G), RS1000249118 (12:62599107 T>A,C), RS1000263170 (12:62592006 C>A), RS1000286814 (12:62599804 A>G), RS1000290456 (12:62551300 T>C)

Disease associations

OMIM: gene MIM:616822 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

4 associations (top):

Study	Trait	p-value
GCST002379_4	Pyoderma gangrenosum in inflammatory bowel disease	5.000000e-06
GCST010244_373	Triglyceride levels	7.000000e-11
GCST90020025_93	Waist-to-hip ratio adjusted for BMI	6.000000e-09
GCST90020027_1672	Waist-hip index	1.000000e-08

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0006835	pyoderma gangrenosum
EFO:0004530	triglyceride measurement
EFO:0007788	BMI-adjusted waist-hip ratio

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4105804 (SINGLE PROTEIN)

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

ChEMBL bioactivities

4 potent at pChembl≥5 of 4 total, top 4 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.42	Kd	3.821	nM	CHEMBL3752910
8.42	ED50	3.821	nM	CHEMBL3752910
6.72	Kd	191.3	nM	CHEMBL5653589
6.72	ED50	191.3	nM	CHEMBL5653589

PubChem BioAssay actives

2 with measured affinity, of 6 total; 2 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
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148763: Binding affinity to human MON2 incubated for 45 mins by Kinobead based pull down assay	kd	0.0038	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148763: Binding affinity to human MON2 incubated for 45 mins by Kinobead based pull down assay	kd	0.1913	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Endosulfan	decreases expression, increases expression	3
Cadmium Chloride	increases expression, decreases expression, increases abundance	3
Nickel	decreases expression	2
aristolochic acid I	decreases expression	1
FR900359	decreases phosphorylation	1
TAK-243	decreases sumoylation	1
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, decreases expression, increases oxidation, increases abundance	1
bisphenol A	decreases expression	1
titanium dioxide	decreases methylation, increases expression	1
decabromobiphenyl ether	decreases expression	1
methylparaben	increases expression	1
sodium arsenite	increases expression	1
butyraldehyde	decreases expression	1
tetrabromobisphenol A	decreases expression	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
methacrylaldehyde	increases oxidation, increases abundance, affects cotreatment, decreases expression	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
pentanal	decreases expression	1
perfluorooctane sulfonic acid	decreases expression	1
CGP 52608	affects binding, increases reaction	1
pentabrominated diphenyl ether 100	decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
bisphenol S	decreases methylation	1
jinfukang	decreases expression	1
Resveratrol	affects cotreatment, increases expression	1
Zoledronic Acid	increases expression	1
Acrolein	affects cotreatment, decreases expression, increases oxidation, increases abundance	1
Air Pollutants	increases oxidation, affects cotreatment, decreases expression, increases abundance	1
Arsenic	increases methylation	1

ChEMBL screening assays

2 unique, capped per target: 2 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4012584	Binding	Binding affinity to MON2 protein in human INA-6 cells after 3 hrs by nanoLC-MS/MS method	Ugi Reaction-Derived α-Acyl Aminocarboxamides Bind to Phosphatidylinositol 3-Kinase-Related Kinases, Inhibit HSF1-Dependent Heat Shock Response, and Induce Apoptosis in Multiple Myeloma Cells. — J Med Chem

Clinical trials (associated diseases)

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