MEN1

Summary

MEN1 (menin 1, HGNC:7010) is a protein-coding gene on chromosome 11q13.1, encoding Menin (O00255). Essential component of a MLL/SET1 histone methyltransferase (HMT) complex, a complex that specifically methylates ‘Lys-4’ of histone H3 (H3K4). It is a selective cancer dependency (DepMap: 29.3% of cell lines) and haploinsufficient (ClinGen: sufficient evidence).

This gene encodes menin, a tumor suppressor associated with a syndrome known as multiple endocrine neoplasia type 1. Menin is a scaffold protein that functions in histone modification and epigenetic gene regulation. It is thought to regulate several pathways and processes by altering chromatin structure through the modification of histones.

Source: NCBI Gene 4221 — RefSeq curated summary.

At a glance

• Gene–disease (curated): multiple endocrine neoplasia type 1 (Definitive, ClinGen) — +3 more curated relationships
• GWAS associations: 1
• Clinical variants (ClinVar): 3,125 total — 470 pathogenic, 147 likely-pathogenic
• Phenotypes (HPO): 177
• Druggable target: yes — 475 molecules with ChEMBL bioactivity
• Cancer driver (intOGen): loss-of-function (tumor-suppressor-like) across 8 cancer types
• Cancer dependency (DepMap): dependent in 29.3% of screened cell lines
• Dosage sensitivity (ClinGen): haploinsufficiency sufficient evidence, triplosensitivity no evidence
• Transcription factor: yes — 12 downstream targets (CollecTRI)
• MANE Select transcript: NM_001370259

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:7010
Approved symbol	MEN1
Name	menin 1
Location	11q13.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000133895
Ensembl biotype	protein_coding
OMIM	613733
Entrez	4221

Gene structure

Transcript identifiers

Ensembl transcripts: 42 — 37 protein_coding, 3 retained_intron, 2 nonsense_mediated_decay

ENST00000312049, ENST00000315422, ENST00000377313, ENST00000377316, ENST00000377321, ENST00000377326, ENST00000394374, ENST00000394376, ENST00000413626, ENST00000424912, ENST00000429702, ENST00000440873, ENST00000450708, ENST00000478548, ENST00000671939, ENST00000671965, ENST00000672079, ENST00000672304, ENST00000710881, ENST00000864594, ENST00000864595, ENST00000864596, ENST00000864597, ENST00000864598, ENST00000864599, ENST00000864600, ENST00000864601, ENST00000864602, ENST00000917699, ENST00000917700, ENST00000917701, ENST00000917702, ENST00000917703, ENST00000917704, ENST00000917705, ENST00000917706, ENST00000917707, ENST00000917708, ENST00000917709, ENST00000917710, ENST00000917711, ENST00000962403

RefSeq mRNA: 24 — MANE Select: NM_001370259 NM_000244, NM_001370251, NM_001370259, NM_001370260, NM_001370261, NM_001370262, NM_001370263, NM_001407142, NM_001407143, NM_001407144, NM_001407145, NM_001407146, NM_001407147, NM_001407148, NM_001407149, NM_001407150, NM_001407151, NM_001407152, NM_130799, NM_130800, NM_130801, NM_130802, NM_130803, NM_130804

CCDS: CCDS31600, CCDS8083, CCDS91503, CCDS91504

Canonical transcript exons

ENST00000450708 — 10 exons

Exon	Start	End
ENSE00000000333	64810514	64810551
ENSE00001171239	64806232	64806368
ENSE00001171248	64807011	64807098
ENSE00001171254	64807179	64807219
ENSE00001298138	64809665	64810132
ENSE00001312579	64807891	64808099
ENSE00003617827	64805635	64805770
ENSE00003685663	64805034	64805198
ENSE00003789012	64807552	64807680
ENSE00004012581	64803516	64804816

Expression profiles

Bgee: expression breadth ubiquitous, 271 present calls, max score 91.07.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 16.8524 / max 91.6704, expressed in 1777 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
120468	15.3967	1754
120469	1.0761	636
120470	0.3797	177

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
granulocyte	CL:0000094	91.07	gold quality
lower esophagus mucosa	UBERON:0035834	90.45	gold quality
right hemisphere of cerebellum	UBERON:0014890	89.74	gold quality
right adrenal gland	UBERON:0001233	89.18	gold quality
ganglionic eminence	UBERON:0004023	89.11	gold quality
ventricular zone	UBERON:0003053	88.94	gold quality
cerebellar hemisphere	UBERON:0002245	88.85	gold quality
mucosa of transverse colon	UBERON:0004991	88.76	gold quality
right adrenal gland cortex	UBERON:0035827	88.74	gold quality
cerebellar cortex	UBERON:0002129	88.72	gold quality
right lobe of liver	UBERON:0001114	88.45	gold quality
right lobe of thyroid gland	UBERON:0001119	88.40	gold quality
left adrenal gland	UBERON:0001234	88.08	gold quality
stromal cell of endometrium	CL:0002255	88.01	gold quality
cortical plate	UBERON:0005343	87.98	gold quality
right frontal lobe	UBERON:0002810	87.97	gold quality
left lobe of thyroid gland	UBERON:0001120	87.92	gold quality
left adrenal gland cortex	UBERON:0035825	87.92	gold quality
metanephros cortex	UBERON:0010533	87.68	gold quality
cerebellum	UBERON:0002037	87.65	gold quality
right ovary	UBERON:0002118	87.62	gold quality
adrenal cortex	UBERON:0001235	87.24	gold quality
adenohypophysis	UBERON:0002196	87.20	gold quality
embryo	UBERON:0000922	87.09	gold quality
body of stomach	UBERON:0001161	87.09	gold quality
skin of leg	UBERON:0001511	86.90	gold quality
pituitary gland	UBERON:0000007	86.88	gold quality
skin of abdomen	UBERON:0001416	86.88	gold quality
body of pancreas	UBERON:0001150	86.86	gold quality
spleen	UBERON:0002106	86.86	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.04

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

12 targets.

Target	Regulation
BRCA1	Unknown
CASP8	Activation
CDKN1B	Activation
CDKN2C	Repression
GAST	Repression
GATA3	Unknown
HOXA9	Activation
JUND	Repression
PRL	Unknown
RAD51	Unknown
RAD51AP1	Unknown
TERT	Repression

Upstream regulators (CollecTRI, top): EZH2, FOXO1, HIF1A, JUN, KMT2A, MAFK, MNX1, MYC, SMAD7, SP1, TCF23, WT1

miRNA regulators (miRDB)

59 targeting MEN1, 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-6077	99.99	68.04	2299
HSA-MIR-4487	99.96	64.58	1252
HSA-MIR-5688	99.96	73.23	4504
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-552-5P	99.93	68.56	1583
HSA-MIR-4492	99.87	68.25	3611
HSA-MIR-4698	99.84	71.41	4303
HSA-MIR-8076	99.78	68.52	1170
HSA-MIR-4320	99.75	65.80	793
HSA-MIR-4516	99.61	67.78	3390
HSA-MIR-24-3P	99.59	69.97	1934
HSA-MIR-762	99.58	66.61	1994
HSA-MIR-516B-5P	99.56	66.33	1495
HSA-MIR-7106-5P	99.53	67.47	3574
HSA-MIR-4437	99.52	65.29	1266
HSA-MIR-486-3P	99.51	66.82	1901
HSA-MIR-4498	99.47	67.42	2360
HSA-MIR-1275	99.47	67.90	2749
HSA-MIR-6839-3P	99.39	68.86	1301
HSA-MIR-4505	99.27	67.81	2678
HSA-MIR-149-5P	99.25	67.16	1315
HSA-MIR-5787	99.22	67.86	2628
HSA-MIR-6799-5P	99.14	65.72	2093
HSA-MIR-5001-5P	99.05	66.76	1972
HSA-MIR-6506-5P	99.04	65.66	1386
HSA-MIR-6846-5P	98.81	65.86	1121
HSA-MIR-6848-5P	98.81	65.49	1126
HSA-MIR-4656	98.79	66.22	1306
HSA-MIR-3135B	98.61	65.33	1470
HSA-MIR-619-5P	98.57	64.97	1988

Functional genomics

ClinGen dosage: haploinsufficiency 3 (sufficient evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map DepMap (CRISPR cell-line fitness): dependent in 29.3% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• Germline mutations of the MEN1 gene in patients with MEN1 and related disorders are summarized and discussed from a clinical point of view. (PMID:11740047)
• Loss of heterozygosity of the MEN1 gene in a large series of TSH-secreting pituitary adenomas. (PMID:11765049)
• Multiple endocrine neoplasia type 1Burin from Mauritius: a novel MEN1 mutation. (PMID:11765051)
• role in familial hyperaldosteronism (PMID:11903322)
• molecular analyses of multiple endocrine neoplasias (PMID:11956591)
• Frequent occurrence of an intron 4 mutation in multiple endocrine neoplasia type 1. (PMID:12050235)
• Results provide the largest series of MEN1 mutations published to date, which will be a useful tool for further studies focusing on the functional effects of missense mutations. (PMID:12112656)
• These results suggest that menin is an atypical GTPase stimulated by nm23. (PMID:12145286)
• Menin’s interaction with glial fibrillary acidic protein and vimentin suggests a role for the intermediate filament network in regulating menin activity. (PMID:12169273)
• MEN1 tumor-suppressor protein localizes to telomeres during meiosis. (PMID:12203793)
• conclude that the altered MEN1 gene function is of importance in the development of familial isolated hyperparathyroidism (PMID:12213668)
• novel six-nucleotide insertion in exon 4; speculated the mutations involving only exon 4 of the MEN1 gene might induce development of insulinoma (PMID:12417605)
• The transcriptional activity of prolactin promoter in GH3 cells co-transfected with menin was significantly decreased (PMID:12459032)
• Complex cytogenetic abnormalities including telomeric associations and MEN1 mutation in a pediatric ependymoma (PMID:12505253)
• menin binds to RPA2 and has a role in multiple endocrine neoplasia (PMID:12509449)
• Mutational and gross deletion study, and the correlation with clinical features in Spanish patients (PMID:12746426)
• the first description of the expression pattern of menin in human pancreas in situ (PMID:12915685)
• Five adjacent cis-regulatory regions exist upstream of the promoter, whose activity depends partly on a downstream sequence DR1. (PMID:14516745)
• Menin is important for recruiting an mSin3A-histone deacetylase complex to repress JunD transcriptional activity. (PMID:14559791)
• genotype phenotype analysis in familial isolated hyperparathyroidism (PMID:14985373)
• MEN1 associates with a trithorax histone methyltransferase complex and with the Hoxc8 locus. (PMID:14992727)
• Menin inactivation leads to loss of transforming growth factor beta signaling resulting in parathyroid tumorigenesis (PMID:15026366)
• the smad pathway and the tumor suppressor menin are key regulators of activin effects on PRL and Pit-1 expression, as well as on cell growth inhibition (PMID:15031321)
• menin contributes to proliferation control in intestinal epithelial cells (PMID:15054094)
• Presence of multiple developmental aberrations in MEN1 pancreas potentially serve as precursor material for neuroendocrine tumors. (PMID:15070966)
• menin and TGF-beta/Smad3 negatively regulate the BMP-2/Smad1/5- and Runx2-induced transcriptional activities leading to inhibition of cell differentiation (PMID:15150273)
• studies link menin with the MLL histone methyltransferase machinery, with implications for Hox gene expression in leukemia pathogenesis (PMID:15199122)
• a novel mutation of the MEN1 gene may have a role in multiple endocrine neoplasia type 1 (PMID:15205994)
• Obligatory MEN1 gene carrier status did not show a harmful effect on survival in this retrospective analysis tracing back to almost 300 yr. (PMID:15240620)
• Menin missense mutants associated with multiple endocrine neoplasia type 1 are rapidly degraded via the ubiquitin-proteasome pathway (PMID:15254225)
• Menin-JunD interaction may negatively regulate the enhancing effect of menin on c-Jun-mediated transactivation (PMID:15256779)
• Heterozygous germline mutations of MEN1 gene are responsible for MEN1 disorders. Various types of mutations likely causing loss of the gene function have been identified throughout the entire region in patients with MEN1 and related disorders. Review. (PMID:15281352)
• menin has a role in directly binding to DNA and regulation of cell proliferation (PMID:15331604)
• menin suppresses osteoblast maturation, in part, by inhibiting the differentiation actions of JunD (PMID:15563473)
• Routine germline MEN1 mutation testing of all cases of “classical” MEN1, familial hyperparathyroidism, and sporadic hyperparathyroidism with one other MEN1 related condition is justified by national testing services. (PMID:15635078)
• that regulation of cyclin-dependent kinase inhibitor transcription by cooperative interaction between menin and MLL plays a central role in menin’s activity as a tumor suppressor (PMID:15640349)
• Study demonstrates that alterations in the MEN1 gene are involved in about half of all sporadic gastrinomas. (PMID:15944766)
• MEN1 is an essential oncogenic cofactor for MLL-associated leukemogenesis. (PMID:16239140)
• The loss of function of the MEN1 gene is the cause of multiple endocrine neoplasia type 1. (PMID:16324211)
• A novel germline base-pair deletion in exon 7, codon 311 (ACC–>AC) was detected in a case of MEN I. (PMID:16368411)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	men1	ENSDARG00000089456
mus_musculus	Men1	ENSMUSG00000024947
rattus_norvegicus	Men1	ENSRNOG00000021054
drosophila_melanogaster	Mnn1	FBGN0031885

Protein

Protein identifiers

Menin — O00255 (reviewed: O00255)

All UniProt accessions (9): A0A5F9ZHS3, A0A5F9ZI68, A0A8C8KI51, O00255, A0A8C8KI72, A0AA75I0P0, E7EN32, E7ENS2, Q9GZQ5

UniProt curated annotations — full annotation on UniProt →

Function. Essential component of a MLL/SET1 histone methyltransferase (HMT) complex, a complex that specifically methylates ‘Lys-4’ of histone H3 (H3K4). Functions as a transcriptional regulator. Binds to the TERT promoter and represses telomerase expression. Plays a role in TGFB1-mediated inhibition of cell-proliferation, possibly regulating SMAD3 transcriptional activity. Represses JUND-mediated transcriptional activation on AP1 sites, as well as that mediated by NFKB subunit RELA. Positively regulates HOXC8 and HOXC6 gene expression. May be involved in normal hematopoiesis through the activation of HOXA9 expression. May be involved in DNA repair.

Subunit / interactions. Component of the MLL-HCF complex, at least composed of KMT2A/MLL1, MEN1, ASH2L, RBBP5, DPY30, WDR5, HCFC1 and HCFC2. Component of the menin-associated histone methyltransferase complex, at least composed of KMT2B/MLL4, MEN1, ASH2L, RBBP5, DPY30 and WDR5. Interacts with POLR2B. Interacts with POLR2A phosphorylated at ‘Ser-5’, but not with the unphosphorylated, nor ‘Ser-2’ phosphorylated POLR2A forms. Interacts with FANCD2 and DBF4. Interacts with JUND (via MBM motif); inhibits the interaction of JUND with MAPK10 and the phosphorylation of JUND by MAP kinases MAPK8 and MAPK10. Interacts with SMAD3, but not with SMAD2, nor SMAD4. Directly interacts with NFKB1, NFKB2 and RELA. Interacts with KMT2A (via MBM motif). The KMT2A-MEN1 complex interacts with PSIP1 with a greater affinity as MEN1 enhances interaction of KMT2A with PSIP1. Interacts with the fusion protein KMT2A-MLLT3.

Subcellular location. Nucleus.

Tissue specificity. Ubiquitous.

Disease relevance. Familial multiple endocrine neoplasia type I (MEN1) [MIM:131100] Autosomal dominant disorder characterized by tumors of the parathyroid glands, gastro-intestinal endocrine tissue, the anterior pituitary and other tissues. Cutaneous lesions and nervous-tissue tumors can exist. Prognosis in MEN1 patients is related to hormonal hypersecretion by tumors, such as hypergastrinemia causing severe peptic ulcer disease (Zollinger-Ellison syndrome, ZES), primary hyperparathyroidism, and acute forms of hyperinsulinemia. The disease is caused by variants affecting the gene represented in this entry. MEN1 inactivating mutations are responsible for hyperfunctioning of the parathyroid glands and subsequent primary hyperparathyroidism. Primary hyperparathyroidism can occur in isolation or in association with multiple endocrine neoplasia.

Isoforms (3)

UniProt ID	Names	Canonical?
O00255-2	1, Short	yes
O00255-1	2, Long
O00255-3	3

RefSeq proteins (24): NP_000235, NP_001357180, NP_001357188, NP_001357189, NP_001357190, NP_001357191, NP_001357192, NP_001394071, NP_001394072, NP_001394073, NP_001394074, NP_001394075, NP_001394076, NP_001394077, NP_001394078, NP_001394079, NP_001394080, NP_001394081, NP_570711, NP_570712, NP_570713, NP_570714, NP_570715, NP_570716 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR007747	Menin	Family

Pfam: PF05053

UniProt features (179 total): sequence variant 112, helix 30, strand 16, mutagenesis site 9, modified residue 3, splice variant 3, region of interest 2, turn 2, chain 1, compositionally biased region 1

Structure

Experimental structures (PDB)

69 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
6O5I	X-RAY DIFFRACTION	1.24
4GQ4	X-RAY DIFFRACTION	1.27
8VA5	X-RAY DIFFRACTION	1.3
9C4Y	X-RAY DIFFRACTION	1.31
9C4W	X-RAY DIFFRACTION	1.4
9C4Z	X-RAY DIFFRACTION	1.4
4OG4	X-RAY DIFFRACTION	1.45
4GPQ	X-RAY DIFFRACTION	1.46
9C4T	X-RAY DIFFRACTION	1.46
9C4V	X-RAY DIFFRACTION	1.47
4OG6	X-RAY DIFFRACTION	1.49
5DB0	X-RAY DIFFRACTION	1.5
9WN9	X-RAY DIFFRACTION	1.5
6OPJ	X-RAY DIFFRACTION	1.5
4OG8	X-RAY DIFFRACTION	1.53
5DB2	X-RAY DIFFRACTION	1.54
5DDB	X-RAY DIFFRACTION	1.54
9C4S	X-RAY DIFFRACTION	1.54
4GQ6	X-RAY DIFFRACTION	1.55
4GQ3	X-RAY DIFFRACTION	1.56
9C4U	X-RAY DIFFRACTION	1.57
8VA6	X-RAY DIFFRACTION	1.57
9C4X	X-RAY DIFFRACTION	1.58
4X5Y	X-RAY DIFFRACTION	1.59
5DD9	X-RAY DIFFRACTION	1.62
5DDC	X-RAY DIFFRACTION	1.62
4OG5	X-RAY DIFFRACTION	1.63
9WKW	X-RAY DIFFRACTION	1.63
5DDF	X-RAY DIFFRACTION	1.66
5DB3	X-RAY DIFFRACTION	1.71

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O00255-F1	85.13	0.74

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): 487, 543, 594

Mutagenesis-validated functional residues (9):

Position	Phenotype
182	reduced interaction with kmt2a.
278	loss of interaction with kmt2a and jund.
285	reduced interaction with kmt2a; when associated with r-288 and r-290.
288	reduced interaction with kmt2a; when associated with r-285 and r-290.
290	reduced interaction with kmt2a; when associated with r-285 and r-288.
319	reduced interaction with kmt2a.
323	reduced interaction with kmt2a.
366	reduced interaction with kmt2a; when associated with a-370.
370	reduced interaction with kmt2a; when associated with a-366.

Function

Pathways and Gene Ontology

Reactome pathways

24 pathways

ID	Pathway
R-HSA-201722	Formation of the beta-catenin:TCF transactivating complex
R-HSA-2173796	SMAD2/SMAD3:SMAD4 heterotrimer regulates transcription
R-HSA-3769402	Deactivation of the beta-catenin transactivating complex
R-HSA-381426	Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)
R-HSA-5626467	RHO GTPases activate IQGAPs
R-HSA-8957275	Post-translational protein phosphorylation
R-HSA-9772755	Formation of WDR5-containing histone-modifying complexes
R-HSA-9976102	Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells)
R-HSA-162582	Signal Transduction
R-HSA-170834	Signaling by TGF-beta Receptor Complex
R-HSA-194315	Signaling by Rho GTPases
R-HSA-195258	RHO GTPase Effectors
R-HSA-195721	Signaling by WNT
R-HSA-201681	TCF dependent signaling in response to WNT
R-HSA-212165	Epigenetic regulation of gene expression
R-HSA-212436	Generic Transcription Pathway
R-HSA-2173793	Transcriptional activity of SMAD2/SMAD3:SMAD4 heterotrimer
R-HSA-392499	Metabolism of proteins
R-HSA-597592	Post-translational protein modification
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)
R-HSA-9006936	Signaling by TGFB family members
R-HSA-9716542	Signaling by Rho GTPases, Miro GTPases and RHOBTB3
R-HSA-9917777	Epigenetic regulation by WDR5-containing histone modifying complexes

MSigDB gene sets: 562 (showing top): GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_RESPONSE_TO_IONIZING_RADIATION, REACTOME_SIGNALING_BY_TGF_BETA_RECEPTOR_COMPLEX, GOBP_REGULATION_OF_PHOSPHORYLATION, GOBP_NEGATIVE_REGULATION_OF_KINASE_ACTIVITY, GOBP_T_CELL_ACTIVATION_INVOLVED_IN_IMMUNE_RESPONSE, GOBP_ALPHA_BETA_T_CELL_DIFFERENTIATION, GOBP_OSTEOBLAST_DIFFERENTIATION, GOBP_REGULATION_OF_TRANSFERASE_ACTIVITY, chr11q13, GOBP_NEGATIVE_REGULATION_OF_MAPK_CASCADE, GOBP_POSITIVE_REGULATION_OF_CELLULAR_RESPONSE_TO_TRANSFORMING_GROWTH_FACTOR_BETA_STIMULUS, GOBP_NEGATIVE_REGULATION_OF_INTRACELLULAR_SIGNAL_TRANSDUCTION, GOBP_CELL_ACTIVATION_INVOLVED_IN_IMMUNE_RESPONSE, GOBP_CD4_POSITIVE_ALPHA_BETA_T_CELL_ACTIVATION

GO Biological Process (21): negative regulation of transcription by RNA polymerase II (GO:0000122), MAPK cascade (GO:0000165), negative regulation of protein phosphorylation (GO:0001933), osteoblast development (GO:0002076), DNA repair (GO:0006281), regulation of transcription by RNA polymerase II (GO:0006357), DNA damage response (GO:0006974), negative regulation of cell population proliferation (GO:0008285), response to UV (GO:0009411), response to gamma radiation (GO:0010332), positive regulation of transforming growth factor beta receptor signaling pathway (GO:0030511), obsolete negative regulation of DNA-binding transcription factor activity (GO:0043433), T-helper 2 cell differentiation (GO:0045064), negative regulation of osteoblast differentiation (GO:0045668), negative regulation of cyclin-dependent protein serine/threonine kinase activity (GO:0045736), negative regulation of cell cycle (GO:0045786), transcription initiation-coupled chromatin remodeling (GO:0045815), negative regulation of DNA-templated transcription (GO:0045892), positive regulation of transcription by RNA polymerase II (GO:0045944), negative regulation of JNK cascade (GO:0046329), chromatin organization (GO:0006325)

GO Molecular Function (10): four-way junction DNA binding (GO:0000400), Y-form DNA binding (GO:0000403), transcription cis-regulatory region binding (GO:0000976), chromatin binding (GO:0003682), double-stranded DNA binding (GO:0003690), protein-macromolecule adaptor activity (GO:0030674), phosphoprotein binding (GO:0051219), R-SMAD binding (GO:0070412), DNA binding (GO:0003677), protein binding (GO:0005515)

GO Cellular Component (14): chromosome, telomeric region (GO:0000781), chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), endoplasmic reticulum lumen (GO:0005788), cytosol (GO:0005829), nuclear matrix (GO:0016363), transcription repressor complex (GO:0017053), cleavage furrow (GO:0032154), protein-containing complex (GO:0032991), histone methyltransferase complex (GO:0035097), MLL1/2 complex (GO:0044665), MLL1 complex (GO:0071339)

Reactome top-level categories

Rollup of top-16 pathways:

Category	Pathways
TCF dependent signaling in response to WNT	2
Metabolism of proteins	2
Gene expression (Transcription)	2
Transcriptional activity of SMAD2/SMAD3:SMAD4 heterotrimer	1
RHO GTPase Effectors	1
Post-translational protein modification	1
Epigenetic regulation by WDR5-containing histone modifying complexes	1
Differentiation of T cells	1
Signaling by TGFB family members	1
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	1
Signaling by Rho GTPases	1
Signal Transduction	1
Signaling by WNT	1
RNA Polymerase II Transcription	1
Signaling by TGF-beta Receptor Complex	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	5
transcription by RNA polymerase II	3
regulation of transcription by RNA polymerase II	2
osteoblast differentiation	2
regulation of DNA-templated transcription	2
negative regulation of cellular process	2
DNA secondary structure binding	2
binding	2
protein binding	2
nuclear lumen	2
negative regulation of DNA-templated transcription	1
intracellular signaling cassette	1
regulation of protein phosphorylation	1
protein phosphorylation	1
negative regulation of protein modification process	1
negative regulation of phosphorylation	1
cell development	1
DNA metabolic process	1
DNA damage response	1
cellular response to stress	1
cell population proliferation	1
regulation of cell population proliferation	1
response to light stimulus	1
response to ionizing radiation	1
transforming growth factor beta receptor signaling pathway	1
regulation of transforming growth factor beta receptor signaling pathway	1
positive regulation of transmembrane receptor protein serine/threonine kinase signaling pathway	1
positive regulation of cellular response to transforming growth factor beta stimulus	1
alpha-beta T cell activation involved in immune response	1
T cell differentiation involved in immune response	1
type 2 immune response	1
T-helper cell differentiation	1
negative regulation of cell differentiation	1
regulation of osteoblast differentiation	1
regulation of cyclin-dependent protein serine/threonine kinase activity	1
cyclin-dependent protein serine/threonine kinase activity	1
negative regulation of cell cycle	1
negative regulation of protein serine/threonine kinase activity	1
negative regulation of cyclin-dependent protein kinase activity	1
cell cycle	1

Protein interactions and networks

STRING

3848 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MEN1	JUND	P17535	991
MEN1	KMT2A	Q03164	990
MEN1	PSIP1	O75475	986
MEN1	SMAD3	P84022	954
MEN1	CDC73	Q6P1J9	903
MEN1	ESR1	P03372	894
MEN1	FANCD2	Q9BXW9	882
MEN1	GAST	P01350	845
MEN1	PTH	P01270	840
MEN1	PYGM	P11217	830
MEN1	RBBP5	Q15291	828
MEN1	RET	P07949	828
MEN1	FOXN3	O00409	819
MEN1	DAXX	Q9UER7	817
MEN1	ATRX	P46100	800

IntAct

87 interactions, top by confidence:

A	B	Type	Score
MEN1	WDR5	psi-mi:“MI:0915”(physical association)	0.710
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
WDR5	MEN1	psi-mi:“MI:0914”(association)	0.710
KMT2A	MEN1	psi-mi:“MI:0914”(association)	0.640
BRAF	MEN1	psi-mi:“MI:0914”(association)	0.600
MEN1	BRAF	psi-mi:“MI:0915”(physical association)	0.600
MEN1	BRAF	psi-mi:“MI:2364”(proximity)	0.600
MEN1	MYH9	psi-mi:“MI:0915”(physical association)	0.560
MEN1	MYH9	psi-mi:“MI:0403”(colocalization)	0.560
CD226	MEN1	psi-mi:“MI:0914”(association)	0.530
MEN1	FANCD2	psi-mi:“MI:0915”(physical association)	0.520
FANCD2	MEN1	psi-mi:“MI:0915”(physical association)	0.520
NFKB1	MEN1	psi-mi:“MI:0915”(physical association)	0.520
MEN1	NFKB1	psi-mi:“MI:0915”(physical association)	0.520
TP53	MEN1	psi-mi:“MI:0914”(association)	0.480
MEN1	TP53	psi-mi:“MI:2364”(proximity)	0.480
KMT2B	MEN1	psi-mi:“MI:0914”(association)	0.460
H3C1	SMCHD1	psi-mi:“MI:2364”(proximity)	0.410
MEN1	FOXM1	psi-mi:“MI:0915”(physical association)	0.400
MEN1	NR1H3	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (1291): MEN1 (Affinity Capture-MS), TCF7L2 (Affinity Capture-Western), TCF7L2 (Reconstituted Complex), MEN1 (Proximity Label-MS), MEN1 (Proximity Label-MS), MEN1 (Affinity Capture-MS), MEN1 (Affinity Capture-MS), MEN1 (Affinity Capture-MS), MEN1 (Affinity Capture-MS), MEN1 (Affinity Capture-MS), MEN1 (Affinity Capture-MS), MEN1 (Affinity Capture-MS), MEN1 (Phenotypic Enhancement), FANCA (Affinity Capture-Luminescence), RPRM (Affinity Capture-MS)

ESM2 similar proteins: A0JPH4, A2AWP8, A2RRU4, A2SXS5, A4D2P6, A6QM06, D4A6L0, E1BBQ2, E9Q6C8, F1LQY6, O00255, O88559, O94827, P29590, P56726, P97260, P97698, Q0GA42, Q0P5I0, Q0VF94, Q12770, Q17RQ9, Q29RM4, Q49LS8, Q5GH57, Q5GH73, Q5MNU5, Q5SNT2, Q5T848, Q69Z89, Q6DVA0, Q6GQT6, Q6IEE7, Q70EL4, Q8BUM9, Q8C190, Q8C419, Q8NC56, Q8TCT7, Q91ZP9

Diamond homologs: A2SXS5, O00255, O88559, Q0P5I0, Q9WVR8

SIGNOR signaling

13 interactions.

A	Effect	B	Mechanism
MEN1	down-regulates	TERT
MEN1	up-regulates	FANCD2	binding
MEN1	down-regulates	RELA	binding
MEN1	down-regulates	NfKb-p65/p50	binding
MEN1	“up-regulates quantity by expression”	CDKN2C	“transcriptional regulation”
MEN1	“up-regulates quantity by expression”	CDKN1B	“transcriptional regulation”
MEN1	“up-regulates activity”	KMT2A	binding
MEN1	“up-regulates quantity by expression”	HOXA9	methylation
MEN1	“up-regulates activity”	MLL-ENL	binding
MEN1	“up-regulates activity”	MLL-AF9	binding
MEN1	“up-regulates activity”	MLL-AF4	binding
MEN1	up-regulates	Proliferation
MEN1	“up-regulates activity”	“MLL Fusion”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 58 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 WDR5-containing histone-modifying complexes	8	44.3×	3e-09
PKMTs methylate histone lysines	9	30.2×	3e-09
Deactivation of the beta-catenin transactivating complex	5	24.3×	2e-04
Regulation of PD-L1(CD274) transcription	10	22.7×	3e-09
Formation of the beta-catenin:TCF transactivating complex	8	20.0×	6e-07
RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function	8	20.0×	6e-07
Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells)	5	15.2×	7e-04
G2/M DNA damage checkpoint	5	12.5×	1e-03

GO biological processes:

GO term	Partners	Fold	FDR
transcription initiation-coupled chromatin remodeling	6	40.3×	3e-06
positive regulation of miRNA transcription	7	35.7×	8e-07
nucleosome assembly	5	12.3×	3e-03
chromatin remodeling	7	9.0×	1e-03

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: loss-of-function (tumor-suppressor-like) across 8 cancer types — ACC, BLCA, BRCA, HCC, LUNG, PANCREAS, PANET, WDTC.

Clinical variants and AI predictions

ClinVar

3125 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	470
Likely pathogenic	147
Uncertain significance	1216
Likely benign	643
Benign	74

Top pathogenic / likely-pathogenic (30)

Variant ID	HGVS	Classification
1009876	NM_001370259.2(MEN1):c.970_984del (p.Leu324_His328del)	Pathogenic
1059330	NM_001370259.2(MEN1):c.1031C>G (p.Thr344Arg)	Pathogenic
1064409	NM_001370259.2(MEN1):c.201del (p.Ala68fs)	Pathogenic
1068797	NM_001370259.2(MEN1):c.1006dup (p.Glu336fs)	Pathogenic
1069776	NM_001370259.2(MEN1):c.1456G>T (p.Glu486Ter)	Pathogenic
1069786	NM_001370259.2(MEN1):c.238del (p.Val80fs)	Pathogenic
1070314	NM_001370259.2(MEN1):c.936C>A (p.Tyr312Ter)	Pathogenic
1070417	NM_001370259.2(MEN1):c.1010C>A (p.Ala337Asp)	Pathogenic
1070591	NM_001370259.2(MEN1):c.1058_1059insTG (p.Cys354fs)	Pathogenic
1070665	NM_001370259.2(MEN1):c.1013del (p.Leu338fs)	Pathogenic
1070942	NM_001370259.2(MEN1):c.6dup (p.Leu3fs)	Pathogenic
1070954	NM_001370259.2(MEN1):c.1375_1391dup (p.Ala467fs)	Pathogenic
1071830	NM_001370259.2(MEN1):c.117_118del (p.Leu39fs)	Pathogenic
1072112	NM_001370259.2(MEN1):c.1556del (p.Pro519fs)	Pathogenic
1072293	NM_001370259.2(MEN1):c.248_266del (p.Leu83fs)	Pathogenic
1072303	NM_001370259.2(MEN1):c.506_507dup (p.Leu170fs)	Pathogenic
1072314	NM_001370259.2(MEN1):c.1045del (p.Gln349fs)	Pathogenic
1072351	NM_001370259.2(MEN1):c.474del (p.Phe159fs)	Pathogenic
1072612	NM_001370259.2(MEN1):c.831del (p.Met278fs)	Pathogenic
1073205	NM_001370259.2(MEN1):c.1356dup (p.Gln453fs)	Pathogenic
1073347	NM_001370259.2(MEN1):c.1391dup (p.Ala465fs)	Pathogenic
1074463	NM_001370259.2(MEN1):c.269dup (p.Tyr90Ter)	Pathogenic
1074511	NM_001370259.2(MEN1):c.739dup (p.Ile247fs)	Pathogenic
1076266	NM_001370259.2(MEN1):c.1351-1G>T	Pathogenic
1076585	NM_001370259.2(MEN1):c.234dup (p.Pro79fs)	Pathogenic
1331034	NM_001370259.2(MEN1):c.1279_1282dup (p.Pro428fs)	Pathogenic
1358663	NM_001370259.2(MEN1):c.646del (p.Ala216fs)	Pathogenic
1372174	NM_001370259.2(MEN1):c.859G>T (p.Glu287Ter)	Pathogenic
1372620	NM_001370259.2(MEN1):c.1435_1441del (p.Arg479fs)	Pathogenic
1386416	NM_001370259.2(MEN1):c.1660del (p.Gln554fs)	Pathogenic

SpliceAI

1739 predictions. Top by Δscore:

Variant	Effect	Δscore
11:64804812:CGCAC:C	acceptor_gain	1.0000
11:64804815:ACCT:A	acceptor_loss	1.0000
11:64804816:CCT:C	acceptor_loss	1.0000
11:64804823:C:CT	acceptor_gain	1.0000
11:64804824:A:T	acceptor_gain	1.0000
11:64804825:G:GC	acceptor_gain	1.0000
11:64805107:C:A	donor_gain	1.0000
11:64805110:T:TA	donor_gain	1.0000
11:64805114:C:A	donor_gain	1.0000
11:64805194:GTGCC:G	acceptor_gain	1.0000
11:64805195:TGCC:T	acceptor_gain	1.0000
11:64805196:GCC:G	acceptor_gain	1.0000
11:64805197:CC:C	acceptor_gain	1.0000
11:64805197:CCC:C	acceptor_gain	1.0000
11:64805198:CC:C	acceptor_gain	1.0000
11:64805198:CCTGG:C	acceptor_loss	1.0000
11:64805199:C:CC	acceptor_gain	1.0000
11:64805199:CTGGA:C	acceptor_loss	1.0000
11:64805205:G:T	acceptor_gain	1.0000
11:64805629:TTTCA:T	donor_loss	1.0000
11:64805630:TTCAC:T	donor_loss	1.0000
11:64805631:TCACC:T	donor_loss	1.0000
11:64805632:CACC:C	donor_loss	1.0000
11:64805633:ACCT:A	donor_loss	1.0000
11:64805634:CCT:C	donor_loss	1.0000
11:64805634:CCTGG:C	donor_gain	1.0000
11:64805646:C:CA	donor_gain	1.0000
11:64805647:C:A	donor_gain	1.0000
11:64805687:T:TA	donor_gain	1.0000
11:64805766:TGTAG:T	acceptor_gain	1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000294408 (11:64805777 G>A,C), RS1001422615 (11:64806622 C>T), RS1001572990 (11:64813088 C>A,T), RS1001813172 (11:64806153 C>A,G,T), RS1002043285 (11:64809072 G>A), RS1002119318 (11:64807760 G>A,T), RS1002521610 (11:64809358 C>T), RS1002540892 (11:64804238 C>T), RS1003373774 (11:64809396 T>C), RS1003921769 (11:64808316 G>A), RS1003923411 (11:64808627 T>C), RS1005145429 (11:64803212 C>G,T), RS1005396452 (11:64809595 G>A,C,T), RS1006317032 (11:64805964 A>C), RS1006536599 (11:64810031 G>A,C,T)

Disease associations

OMIM: gene MIM:613733 | disease phenotypes: MIM:131100, MIM:617540, MIM:167000, MIM:145000, MIM:102200, MIM:606764, MIM:219090

GenCC curated gene-disease

Disease	Classification	Inheritance
multiple endocrine neoplasia type 1	Definitive	Autosomal dominant
pituitary gigantism	Supportive	Autosomal dominant
familial isolated hyperparathyroidism	Supportive	Autosomal dominant
hereditary pheochromocytoma-paraganglioma	Limited	Autosomal dominant

ClinGen Gene-Disease Validity (1)

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

Disease	Classification	Inheritance
multiple endocrine neoplasia type 1	Definitive	AD

Mondo (27): multiple endocrine neoplasia type 1 (MONDO:0007540), hereditary neoplastic syndrome (MONDO:0015356), hyperparathyroidism (MONDO:0001741), pituitary adenoma 5, multiple types (MONDO:0054601), endocrine gland neoplasm (MONDO:0002082), ovarian cancer (MONDO:0008170), adrenal cortex adenoma (MONDO:0003924), hyperparathyroidism 1 (MONDO:0007767), hereditary breast ovarian cancer syndrome (MONDO:0003582), primary hyperparathyroidism (MONDO:0010837), lung carcinoid tumor (MONDO:0006041), growth hormone secreting pituitary adenoma 1 (MONDO:0007052), diabetes mellitus (MONDO:0005015), hypertensive disorder (MONDO:0005044), parathyroid gland adenoma (MONDO:0006890)

Orphanet (17): Inherited cancer-predisposing syndrome (Orphanet:140162), Multiple endocrine neoplasia type 1 (Orphanet:652), Tumor of endocrine glands (Orphanet:182130), Rare ovarian cancer (Orphanet:213500), Familial isolated hyperparathyroidism (Orphanet:99879), Hereditary breast and/or ovarian cancer syndrome (Orphanet:145), Familial isolated pituitary adenoma (Orphanet:314777), Acromegaly (Orphanet:963), Gastrointestinal stromal tumor (Orphanet:44890), Multiple endocrine neoplasia (Orphanet:276161), Ependymoma (Orphanet:251636), Medullary thyroid carcinoma (Orphanet:1332), Insulinoma (Orphanet:97279), Cushing disease (Orphanet:96253), Pituitary gigantism (Orphanet:99725)

HPO phenotypes

177 total (30 of 177 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000026	Male hypogonadism
HP:0000044	Hypogonadotropic hypogonadism
HP:0000083	Renal insufficiency
HP:0000098	Tall stature
HP:0000121	Nephrocalcinosis
HP:0000134	Female hypogonadism
HP:0000135	Hypogonadism
HP:0000140	Abnormality of the menstrual cycle
HP:0000141	Amenorrhea
HP:0000169	Gingival fibromatosis
HP:0000280	Coarse facial features
HP:0000303	Mandibular prognathia
HP:0000364	Hearing abnormality
HP:0000504	Abnormality of vision
HP:0000508	Ptosis
HP:0000529	Progressive visual loss
HP:0000618	Blindness
HP:0000651	Diplopia
HP:0000708	Atypical behavior
HP:0000716	Depression
HP:0000736	Short attention span
HP:0000739	Anxiety
HP:0000771	Gynecomastia
HP:0000787	Nephrolithiasis
HP:0000802	Impotence
HP:0000822	Hypertension
HP:0000823	Delayed puberty
HP:0000825	Hyperinsulinemic hypoglycemia
HP:0000830	Anterior hypopituitarism

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST001163_5	Urate levels	6.000000e-11

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004531	urate measurement

MeSH disease descriptors (16)

Descriptor	Name	Tree numbers
D049913	ACTH-Secreting Pituitary Adenoma	C04.557.470.035.012; C04.588.322.609.145; C10.228.140.617.738.675.149; C19.344.609.145; C19.700.734.145
D018246	Adrenocortical Adenoma	C04.588.322.078.265.500; C19.053.098.265.500; C19.053.347.500.500; C19.344.078.265.500
D003920	Diabetes Mellitus	C18.452.394.750; C19.246
D004806	Ependymoma	C04.557.465.625.600.380.290; C04.557.470.670.380.290; C04.557.580.625.600.380.290
D046152	Gastrointestinal Stromal Tumors	C04.557.450.565.370; C06.301.371.308; C06.405.249.308
D005877	Gigantism	C05.116.099.492; C05.116.132.479; C19.700.355.528
D061325	Hereditary Breast and Ovarian Cancer Syndrome	C04.588.180.483; C04.588.322.455.431; C04.700.517; C12.050.351.500.056.630.705.431; C12.050.351.937.418.685.431; C12.100.250.056.630.705.431; C12.900.418.685.431; C16.320.700.517; C17.800.090.500.483; C19.344.410.431; C19.391.630.705.431
D006961	Hyperparathyroidism	C19.642.355
D049950	Hyperparathyroidism, Primary	C19.642.355.239
D006973	Hypertension	C14.907.489
D009377	Multiple Endocrine Neoplasia	C04.588.322.400; C04.651.600; C04.700.630; C16.320.700.630; C19.344.400
D018761	Multiple Endocrine Neoplasia Type 1	C04.588.322.400.500; C04.651.600.500; C04.700.630.500; C16.320.700.630.500; C19.344.400.500
D009386	Neoplastic Syndromes, Hereditary	C04.700; C16.320.700
D009447	Neuroblastoma	C04.557.465.625.600.590.650.550; C04.557.470.670.590.650.550; C04.557.580.625.600.590.650.550
D010051	Ovarian Neoplasms	C04.588.322.455; C12.050.351.500.056.630.705; C12.050.351.937.418.685; C12.100.250.056.630.705; C12.900.418.685; C19.344.410; C19.391.630.705
C564166	Hyperparathyroidism 1 (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL1615381 (SINGLE PROTEIN), CHEMBL2093861 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

475 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 978,785 (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
CHEMBL841	LOPERAMIDE	4	22,587
CHEMBL1014	CANDESARTAN CILEXETIL	4	11,194
CHEMBL1015	EVANS BLUE FREE ACID	4	26
CHEMBL1018	DIENESTROL	4	5,607
CHEMBL1023	BEXAROTENE	4	40,951
CHEMBL1024	IFOSFAMIDE	4	139,212
CHEMBL103	PROGESTERONE	4	162,141
CHEMBL104	CLOTRIMAZOLE	4	56,325
CHEMBL1046	AMINOCAPROIC ACID	4	95,343
CHEMBL1051	LATANOPROST	4	14,975
CHEMBL1057	FLUORESCEIN	4	329,940
CHEMBL1068	OXCARBAZEPINE	4	16,118
CHEMBL1082607	SALMETEROL XINAFOATE	4	15,201
CHEMBL1083993	AMIODARONE HYDROCHLORIDE	4	3,265
CHEMBL1086440	TRICLABENDAZOLE	4	4,136
CHEMBL1089641	TRYPAN BLUE FREE ACID	4	113
CHEMBL110458	MIGALASTAT	4	430
CHEMBL1108	DROPERIDOL	4	16,888
CHEMBL1112	ARIPIPRAZOLE	4	24,205
CHEMBL1113	AMOXAPINE	4	20,128
CHEMBL1116	RALOXIFENE HYDROCHLORIDE	4
CHEMBL1117	IDARUBICIN	4
CHEMBL112	ACETAMINOPHEN	4
CHEMBL1133	OXYBUTYNIN CHLORIDE	4
CHEMBL1134	DECAMETHONIUM BROMIDE	4
CHEMBL1172	DESLORATADINE	4
CHEMBL1185568	DITHIAZANINE	4
CHEMBL119	TRIMETREXATE	4
CHEMBL1200326	NICARDIPINE HYDROCHLORIDE	4
CHEMBL1200332	PROTRIPTYLINE HYDROCHLORIDE	4

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

Binding affinities (BindingDB)

292 measured of 361 human assays (361 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
US20250197392, Compound 51a	IC50	0.024 nM	US-20250197392: CRYSTALLINE FORMS OF AN INHIBITOR OF THE MENIN/MLL INTERACTION
2-[3-[[(3R)-1-[(1-acetylpiperidin-4-yl)methyl]pyrrolidin-3-yl]methyl]-4-methylpyrrolo[2,3-c]pyridin-1-yl]-5-fluoro-N-methyl-N-propan-2-ylbenzamide	IC50	0.042 nM	US-20250197392: CRYSTALLINE FORMS OF AN INHIBITOR OF THE MENIN/MLL INTERACTION
CHEMBL4211366	IC50	1 nM
(R)-2-((5-(2-(6-amino-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-3-chloro-1,2,4-triazin-6-yl)oxy)-N-ethyl-5-fluoro-N-isopropylbenzamide	IC50	33 nM	US-12473295: Substituted straight chain spiro derivatives
(R)-N-ethyl-5-fluoro-N-isopropyl-2-((3-methoxy-5-(2-(6-((2-methoxyethyl)(methyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide formate	IC50	35 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[[(2R)-1-methoxypropan-2-yl]amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	49 nM	US-12473295: Substituted straight chain spiro derivatives
(R)-N-ethyl-5-fluoro-N-isopropyl-2-((5-(2-(2-methyl-6-((3,3,3-trifluoropropyl)amino)hexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide	IC50	50 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-(3,3-difluoropropylamino)-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	50 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[[(2R)-1-methoxypropan-2-yl]-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	51 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-amino-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-3-methyl-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	51 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R,5R)-5-hydroxy-6-[2-methoxyethyl(methyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	53 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[[(2R)-2-hydroxy-3-methoxypropyl]-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	54 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[(2-methoxy-2-methylpropyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	57 nM	US-12473295: Substituted straight chain spiro derivatives
US12473295, Compound 233	IC50	58 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-2-[[5-[2-[(3R,5R)-6-[ethyl(methyl)amino]-5-hydroxy-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-5-fluoro-N-propan-2-ylbenzamide	IC50	58 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[[(2R)-1-hydroxy-3-methoxypropan-2-yl]-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	60 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-[[(2S)-2,3-dimethoxypropyl]-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	62 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-[[3-(dimethylamino)-3-oxopropyl]-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	63 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-2-methyl-6-[methyl(propan-2-yl)amino]hexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	65 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[2-methoxypropyl(methyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	65 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[2-methoxyethyl(methyl)amino]-2-methylheptan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	66 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-amino-2,6-dimethylheptan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	67 nM	US-12473295: Substituted straight chain spiro derivatives
US12473295, Compound 402	IC50	67 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-1-[(3-amino-3-oxopropyl)amino]-4-methylpentan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	68 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-[[3-(dimethylamino)-3-oxopropyl]-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-5-fluoro-N,N-di(propan-2-yl)benzamide	IC50	70 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[3-methoxypropyl(methyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	71 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-(2,2-dimethoxyethylamino)-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	74 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R,5S)-5-hydroxy-6-[2-methoxyethyl(methyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	77 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-[[3-(dimethylamino)-2-methyl-3-oxopropyl]-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	79 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R,5R)-6-(diethylamino)-5-hydroxy-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	79 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-(dimethylamino)-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-5-fluoro-N,N-di(propan-2-yl)benzamide	IC50	80 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3S)-6-[[3-(dimethylamino)-3-oxopropyl]-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-5-fluoro-N,N-di(propan-2-yl)benzamide	IC50	81 nM	US-12473295: Substituted straight chain spiro derivatives
5-fluoro-2-[4-[2-[(3R)-6-[2-methoxyethyl(methyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]pyridazin-3-yl]oxy-N,N-di(propan-2-yl)benzamide	IC50	83 nM	US-12473295: Substituted straight chain spiro derivatives
5-fluoro-2-[[5-[2-[(3R)-6-[2-methoxyethyl(methyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-methyl-N-propan-2-ylbenzamide	IC50	84 nM	US-12473295: Substituted straight chain spiro derivatives
US12473295, Compound 407	IC50	86 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R,5S)-6-(dimethylamino)-5-hydroxy-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-5-fluoro-N,N-di(propan-2-yl)benzamide	IC50	88 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-2-methyl-6-[methyl(propyl)amino]hexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	89 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[[(2S)-1-hydroxy-3-methoxypropan-2-yl]amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	89 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[(2-hydroxy-2-methylpropyl)-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	93 nM	US-12473295: Substituted straight chain spiro derivatives
(R)-2-((5-(2-(6-(dimethylamino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)-N-ethyl-5-fluoro-N-isopropylbenzamide	IC50	95 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[[(2R)-1-hydroxy-3-methoxypropan-2-yl]amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	96 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R,5R)-6-(dimethylamino)-5-hydroxy-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-5-fluoro-N,N-di(propan-2-yl)benzamide	IC50	97 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-N-isopropyl-2-((5-(2-(6-((2-methoxy-2-methylpropyl)amino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide	IC50	99 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-(6-amino-2-methylhexan-3-yl)-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	100 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-(dimethylamino)-2,6-dimethylheptan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	100 nM	US-12473295: Substituted straight chain spiro derivatives
2-[[5-[2-[(3R)-6-(1,3-dimethoxypropan-2-ylamino)-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-ethyl-5-fluoro-N-propan-2-ylbenzamide	IC50	100 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[(3-hydroxy-2-methoxypropyl)amino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	100 nM	US-12473295: Substituted straight chain spiro derivatives
N-ethyl-5-fluoro-2-[[5-[2-[(3R)-6-[(3-hydroxy-2-methoxypropyl)-methylamino]-2-methylhexan-3-yl]-2,7-diazaspiro[3.4]octan-7-yl]-1,2,4-triazin-6-yl]oxy]-N-propan-2-ylbenzamide	IC50	100 nM	US-12473295: Substituted straight chain spiro derivatives
(R)-N-ethyl-5-fluoro-N-isopropyl-2-((5-(2-(2-methyl-6-(methylamino)hexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)benzamide hydrochloride	IC50	110 nM	US-12473295: Substituted straight chain spiro derivatives
(*R)-2-((5(2-(6-(dimethylamino)-2-methylhexan-3-yl)-2,6-diazaspiro[3.4]octan-6-yl)-1,2,4-triazin-6-yl)oxy)-5-fluoro-N,N-diisopropylbenzamide fumarate	IC50	110 nM	US-12473295: Substituted straight chain spiro derivatives

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
9.98	Ki	0.104	nM	CHEMBL5267644
9.30	IC50	0.5	nM	CHEMBL5272148
9.30	IC50	0.5	nM	CHEMBL5414266
9.29	IC50	0.51	nM	CHEMBL5272148
9.08	IC50	0.83	nM	CHEMBL4216333
9.00	IC50	1	nM	CHEMBL4211366
9.00	IC50	1	nM	CHEMBL4530300
9.00	Ki	1	nM	CHEMBL4585198
9.00	IC50	1	nM	CHEMBL5282452
9.00	IC50	1	nM	CHEMBL6053681
8.85	Kd	1.4	nM	CHEMBL2314822
8.85	Ki	1.4	nM	CHEMBL4551865
8.85	Ki	1.4	nM	CHEMBL4592636
8.77	IC50	1.7	nM	CHEMBL4457657
8.77	Ki	1.7	nM	CHEMBL4449199
8.77	IC50	1.7	nM	CHEMBL5076146
8.70	IC50	2	nM	CHEMBL4454017
8.70	IC50	2	nM	CHEMBL4528467
8.70	IC50	2	nM	CHEMBL4571451
8.70	IC50	2	nM	CHEMBL4553102
8.70	IC50	2	nM	CHEMBL4588924
8.70	IC50	2	nM	CHEMBL4456003
8.70	IC50	2	nM	CHEMBL4456868
8.70	IC50	2	nM	CHEMBL4450979
8.70	Ki	2	nM	CHEMBL4516680
8.70	Ki	2	nM	CHEMBL4522767
8.70	IC50	2	nM	CHEMBL5884894
8.70	IC50	2	nM	CHEMBL5886290
8.70	IC50	2	nM	CHEMBL5983807
8.70	IC50	2	nM	CHEMBL5794245
8.70	IC50	2	nM	CHEMBL5766765
8.70	IC50	2	nM	CHEMBL5864844
8.70	IC50	2	nM	CHEMBL4457657
8.70	IC50	2	nM	CHEMBL5817522
8.63	IC50	2.35	nM	CHEMBL4788214
8.62	Ki	2.4	nM	CHEMBL4578509
8.60	IC50	2.5	nM	CHEMBL5085940
8.59	IC50	2.6	nM	CHEMBL4438797
8.57	Ki	2.7	nM	CHEMBL4444304
8.57	Ki	2.7	nM	CHEMBL4458829
8.57	IC50	2.7	nM	CHEMBL5081367
8.57	IC50	2.7	nM	CHEMBL5094183
8.55	IC50	2.8	nM	CHEMBL5071412
8.55	IC50	2.8	nM	CHEMBL5079678
8.54	Ki	2.9	nM	CHEMBL2314823
8.54	IC50	2.9	nM	CHEMBL5090509
8.52	IC50	3	nM	CHEMBL4466396
8.52	IC50	3	nM	CHEMBL4435830
8.52	IC50	3	nM	CHEMBL5079839
8.52	IC50	3	nM	CHEMBL6047118

PubChem BioAssay actives

435 with measured affinity, of 621 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
N-[3-[[2-cyano-4-methyl-5-[[4-[[2-(methylamino)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]methyl]-1-bicyclo[1.1.1]pentanyl]formamide	1925952: Inhibition of human Menin to MLL protein-protein interaction	ic50	0.0005	uM
N-[3-[[2-cyano-4-methyl-5-[[4-[[2-(methylamino)-6-(3,3,3-trifluoropropyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indol-1-yl]methyl]-1-bicyclo[1.1.1]pentanyl]formamide	1980330: Inhibition of human menin/MLL protein-protein interaction by competition based fluorescence polarization assay	ic50	0.0005	uM
4-[4-(4-chlorophenyl)-3,6-dihydro-2H-pyridin-1-yl]-2-cyclopentyl-2-phenylbutan-1-amine	1925952: Inhibition of human Menin to MLL protein-protein interaction	ic50	0.0008	uM
4-cyclopentyl-2-ethyl-4-[1-[[1-(4-pyridin-4-ylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1,3-dihydroisoquinoline	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0010	uM
[(1S,2R)-2-[(4S)-2-methyl-4-[1-[[1-(4-pyridin-4-ylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1,3-dihydroisoquinolin-4-yl]cyclopentyl] N-methylcarbamate	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0010	uM
(1R,9R)-11-(2-hydroxy-5-phenylpentyl)-2,11-diazatricyclo[7.3.1.02,7]trideca-4,6-dien-3-one	1372683: Displacement of FITC-MBM1 from menin (unknown origin) measured after 1 hr by fluorescence polarization assay	ic50	0.0010	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-[4-[1-[(E)-4-(3,3-difluoroazetidin-1-yl)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0010	uM
(1R,9S)-11-(2-hydroxy-5-phenylpentyl)-1,9-dimethyl-7,11-diazatricyclo[7.3.1.02,7]trideca-2,4-dien-6-one	1925950: Inhibition of Menin to MLL (unknown origin) protein-protein interaction	ic50	0.0010	uM
4-cyclopentyl-2-propan-2-yl-4-[1-[[1-(4-pyridin-4-ylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1,3-dihydroisoquinoline	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0014	uM
4-cyclopentyl-2-(cyclopropylmethyl)-4-[1-[[1-(4-pyridin-4-ylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1,3-dihydroisoquinoline	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0014	uM
N-[2-[2-[2-[2-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(3S,9S,15S,18S,29S)-3-(3-carbamimidamidopropyl)-15-[(3,5-difluorophenyl)methyl]-2,5,8,14,17,28-hexaoxospiro[1,4,7,13,16,27-hexazatricyclo[27.3.0.09,13]dotriacontane-6,1’-cyclobutane]-18-yl]amino]-3-(1H-indol-2-yl)-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-2-oxoethoxy]ethoxy]ethoxy]ethyl]-3’,6’-dihydroxy-3-oxospiro[2-benzofuran-1,9’-xanthene]-5-carboxamide	721766: Binding affinity to menin (unknown origin) after 60 mins by fluorescence polarization assay	kd	0.0014	uM
4-cyclopentyl-4-[1-[[1-(4-pyridin-4-ylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-2,3-dihydro-1H-isoquinoline	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0017	uM
methyl N-[(1S,2R)-2-[(1S)-1-[1-[[1-[4-[1-[(E)-4-(dimethylamino)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-2-(2-ethylimidazol-1-yl)-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0017	uM
methyl N-[(1S,2R)-2-[(1S)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-2-(dimethylamino)-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0017	uM
2-cyclobutyl-4-cyclopentyl-4-[1-[[1-(4-pyridin-4-ylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1,3-dihydroisoquinoline	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0020	uM
4-cyclopentyl-2-methyl-4-[1-[[1-(4-pyridin-4-ylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1,3-dihydroisoquinoline	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0020	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[1-[4-(1-prop-2-enoylazetidin-3-yl)sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0020	uM
methyl N-[(1S,2R)-2-[(1S)-1-[1-[[1-[4-[1-[(E)-4-(dimethylamino)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)-2-(triazol-1-yl)ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0020	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-[4-[1-[(E)-4-(4,4-difluoropiperidin-1-yl)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0020	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[1-[4-[1-[(E)-4-pyrrolidin-1-ylbut-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0020	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-[4-[1-[(E)-4-(3-fluoroazetidin-1-yl)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0020	uM
methyl N-[(1S,2R)-2-[(1S)-1-[1-[[1-[4-[1-[(E)-4-(dimethylamino)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)-2-pyrrolidin-1-ylethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0020	uM
methyl N-[(1S,2R)-2-[(1S)-1-[1-[[1-[4-[1-[(E)-4-(dimethylamino)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)-2-piperidin-1-ylethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0020	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-[4-[1-[(E)-4-(azetidin-1-yl)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0020	uM
1-[1-[[1-(4-cyclohexylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1-cyclopentyl-3,4-dihydro-2H-isoquinoline	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0024	uM
(2S)-1-[(3S,6S,8Z,11S,17S)-6-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamidopropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-[(3-fluorophenyl)methyl]-2,5,13,16-tetraoxospiro[1,4,12,15-tetrazabicyclo[15.3.0]icos-8-ene-14,1’-cyclobutane]-11-carbonyl]-N-[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]pyrrolidine-2-carboxamide	1743094: Inhibition of Menin-MLL protein-protein interaction (unknown origin) preincubated for 1 hr in presence of FLSN-MLL4-43 peptide followed by compound addition and measured after 1 hr by fluorescence polarization assay	ic50	0.0024	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)-3-methoxyazetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0025	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[1-[4-[1-[(E)-4-piperidin-1-ylbut-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0026	uM
4-[2-[4-cyclopentyl-4-[1-[[1-(4-pyridin-4-ylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1,3-dihydroisoquinolin-2-yl]ethyl]morpholine	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0027	uM
[(1S,2R)-2-[(S)-cyano-[1-[[1-(4-cyanophenyl)azetidin-3-yl]methyl]piperidin-4-yl]-phenylmethyl]cyclopentyl] N-methylcarbamate	1568950: Inhibition of FAM-probe binding to Menin (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ki	0.0027	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[[(1S,4S)-5-prop-2-enoyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]sulfonyl]phenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0027	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-[4-[1-[(E)-4-(dimethylamino)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]-3-methoxyazetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0027	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-(1-prop-2-enoylazetidin-3-yl)sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0028	uM
methyl N-[(1S,2R)-2-[(1S)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)-2-pyrrolidin-1-ylethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0028	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)-3-methylazetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0029	uM
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]-N-[2-[[(2S,3R)-1-[[2-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]pyrrolidine-2-carboxamide	721766: Binding affinity to menin (unknown origin) after 60 mins by fluorescence polarization assay	ki	0.0029	uM
methyl N-[(1S,2R)-2-[(S)-cyano-[1-[[1-[4-[1-[(E)-4-(dimethylamino)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-(3-fluorophenyl)methyl]cyclopentyl]carbamate	1568949: Inhibition of fluorescent probe binding to Menin (2 to 610 residues containing deletion from 460-519) (unknown origin) after 60 mins by fluorescence polarization competitive binding assay	ic50	0.0030	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-[4-[1-[(E)-4-(dimethylamino)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0030	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[(3S)-1-prop-2-enoylpiperidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0030	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)-3-fluoroazetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0032	uM
methyl N-[(1S,2R)-2-[(1S)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)-2-morpholin-4-ylethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0034	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0035	uM
methyl N-[(1S,2R)-2-[(1S)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)-2-(4-hydroxy-4-methylpiperidin-1-yl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0035	uM
4-methyl-1-[[(2S)-5-oxomorpholin-2-yl]methyl]-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]piperidin-1-yl]methyl]indole-2-carbonitrile	1375610: Displacement of fluorescein-labeled MLL4-43 from full length human menin expressed in Escherichia coli BL21 (DE3) cells after 3 hrs by fluorescence polarization assay	ic50	0.0036	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-[1-[[1-(4-cyclopropylsulfonylphenyl)-3-hydroxyazetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0036	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-[(3R)-1-prop-2-enoylpiperidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0037	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[3-methoxy-1-[4-(1-prop-2-enoylpiperidin-4-yl)sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0038	uM
[4-[[2-[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]-2,7-diazaspiro[4.4]nonan-7-yl]methyl]phenyl]methanesulfonamide	1354811: Inhibition of biotinylated MLL-1 derived biotinylated Btn-PEG2- PEG2-S-Nva-RWRFPARPGTT-Amide binding to recombinant full length N-terminal His-tagged menin (unknown origin) expressed in Escherichia coli incubated for 10 mins by TR-FRET assay	ic50	0.0040	uM
methyl N-[(1S,2R)-2-[(1S)-2-(azetidin-1-yl)-1-(3-fluorophenyl)-1-[1-[[1-[4-[1-[(E)-4-(4-fluoropiperidin-1-yl)but-2-enoyl]azetidin-3-yl]sulfonylphenyl]azetidin-3-yl]methyl]piperidin-4-yl]ethyl]cyclopentyl]carbamate	1549057: Inhibition of fluorescent labeled tracer binding to Menin (unknown origin) after 1 hr by fluorescence polarization competitive binding assay	ic50	0.0040	uM
methyl N-[(1S,2R)-2-[(1S)-2-amino-1-[1-[[1-(4-cyclopropylsulfonylphenyl)azetidin-3-yl]methyl]piperidin-4-yl]-1-(3-fluorophenyl)ethyl]cyclopentyl]carbamate	1817578: Binding affinity to menin (unknown origin) incubated for 1 hr by fluorescence polarization-based competitive binding assay	ic50	0.0040	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases expression	2
Doxorubicin	affects expression, decreases expression	2
Estradiol	affects binding, decreases reaction, increases expression	2
Valproic Acid	increases expression, increases methylation	2
aristolochic acid I	increases expression	1
FR900359	decreases phosphorylation	1
dicrotophos	increases expression	1
geraniol	increases expression	1
methylselenic acid	affects expression	1
beta-lapachone	decreases expression	1
aflatoxin B2	decreases methylation	1
S-(1,2-dichlorovinyl)cysteine	decreases expression	1
di-n-butylphosphoric acid	affects expression	1
CD 437	decreases expression	1
3-(4’-hydroxy-3’-adamantylbiphenyl-4-yl)acrylic acid	decreases expression	1
abrine	decreases expression	1
bisphenol AF	affects binding, affects folding, increases reaction	1
Sunitinib	decreases expression	1
Leflunomide	decreases expression	1
Air Pollutants	increases abundance, increases expression	1
Benzo(a)pyrene	affects methylation	1
Caffeine	decreases phosphorylation	1
Cisplatin	decreases expression	1
Quercetin	decreases reaction, increases expression	1
Smoke	decreases expression	1
Tamoxifen	decreases response to substance, affects binding, decreases reaction	1
Thiram	decreases expression	1
Tretinoin	decreases expression	1
Metribolone	affects binding, affects folding, decreases reaction	1
Cyclosporine	decreases expression	1

ChEMBL screening assays

93 unique, capped per target: 86 binding, 7 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2320318	Binding	Binding affinity to menin (unknown origin) after 60 mins by fluorescence polarization assay	Structure-based design of high-affinity macrocyclic peptidomimetics to block the menin-mixed lineage leukemia 1 (MLL1) protein-protein interaction. — J Med Chem
CHEMBL5723305	Functional	Affinity Biochemical interaction: (Enzymatic assay) EUB0002767a MEN1	Affinity Biochemical Literature for EUbOPEN Chemogenomic Library

Cellosaurus cell lines

117 cell lines: 99 cancer cell line, 9 induced pluripotent stem cell, 3 transformed cell line, 3 finite cell line, 2 embryonic stem cell, 1 telomerase immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_0395	LNCaP	Cancer cell line	Male
CVCL_1379	LNCaP clone FGC	Cancer cell line	Male
CVCL_3872	LNCaP-CL1	Cancer cell line	Male
CVCL_4782	LNCaP C4-2	Cancer cell line	Male
CVCL_4783	LNCaP C4	Cancer cell line	Male
CVCL_4784	LNCaP C4-2B	Cancer cell line	Male
CVCL_4785	LNCaP C4-2B2	Cancer cell line	Male
CVCL_4786	LNCaP C4-2B3	Cancer cell line	Male
CVCL_4787	LNCaP C4-2B4	Cancer cell line	Male
CVCL_4788	LNCaP C4-2B5	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00037518	PHASE4	COMPLETED	A Study of an Investigational Medication for Severe Primary Hyperparathyroidism or Parathyroid Cancer
NCT00359385	PHASE4	WITHDRAWN	The Effects of Alendronate After Cure of Primary Hyperparathyroidism
NCT00379899	PHASE4	COMPLETED	ADVANCE: Study to Evaluate Cinacalcet Plus Low Dose Vitamin D on Vascular Calcification in Subjects With Chronic Kidney Disease Receiving Hemodialysis
NCT01143987	PHASE4	COMPLETED	Cincalcet and Vascular Arterial Stiffness Among Peritoneal Dialysis Patients With Secondary Hyperparathyroidism
NCT01573520	PHASE4	COMPLETED	Treatment Adhesion in Dialysis Patients Treated With Cinacalcet
NCT00417612	PHASE3	COMPLETED	Effectiveness of Paricalcitol in Reducing Parathyroid Hormone (PTH) Levels in X-linked Hypophosphatemic Rickets
NCT00527267	PHASE3	COMPLETED	Safety and Efficacy Study of AMG 073 in Hemodialysis Subjects
NCT00975000	PHASE3	COMPLETED	Treatment of Autonomous Hyperparathyroidism in Post Renal Transplant Recipients
NCT01191762	PHASE3	COMPLETED	Sevelamer and Secondary Hyperparathyroidism in Chronic Kidney Disease
NCT01277510	PHASE3	TERMINATED	Pediatric Chronic Kidney Disease Safety and Efficacy
NCT04040946	PHASE3	COMPLETED	Trial Comparing 2 Diagnostic Strategies for Preoperative Localization of Parathyroid Adenoma in Primary Hyperparathyroidism:TEMP / CT With Tc99m-sestaMIBI or PET / CT With F18-choline in First Intention
NCT00001277	PHASE2	COMPLETED	Studies of Elevated Parathyroid Activity
NCT00454363	PHASE2	COMPLETED	Pazopanib Hydrochloride in Treating Patients With Advanced Neuroendocrine Cancer
NCT02101918	PHASE2	COMPLETED	Ziv-Aflibercept in Treating and Computed Tomography Perfusion Imaging in Predicting Response in Patients With Pancreatic Neuroendocrine Tumors That Are Metastatic or Cannot Be Removed by Surgery
NCT03950609	PHASE2	ACTIVE_NOT_RECRUITING	Lenvatinib and Everolimus in Treating Patients With Advanced, Unresectable Carcinoid Tumors
NCT01673646	PHASE2	COMPLETED	Efficacy and Safety of Pasireotide LAR (Long-acting Release) in Japanese Patients With Acromegaly or Pituitary Gigantism
NCT00744302	PHASE2	COMPLETED	Study of 1.25 mmol/L Calcium Dialysate on Mineral Metabolism in Haemodialysis Patients.
NCT01656070	PHASE2	COMPLETED	Vitamin D Supplementation in HIV-infected Youth
NCT02432599	PHASE2	COMPLETED	Interest of the F18-choline as a Second Line of the Tracer for Detection of Parathyroid Adenomas
NCT02831179	PHASE1	WITHDRAWN	Veliparib, Capecitabine, and Temozolomide in Patients With Advanced, Metastatic, and Recurrent Neuroendocrine Tumor
NCT00538720	PHASE1	COMPLETED	Effects of Vitamin D Replacement in Patients With Primary Hyperparathyroidism (PHPT)
NCT00573573	PHASE1	UNKNOWN	Energy Specific Far Infrared Radiation Treatment for Hyperparathyroidism
NCT01333267	PHASE1	WITHDRAWN	One Week Comparison Study of PTH and PTHrP Infusions
NCT03050268	Not specified	RECRUITING	Familial Investigations of Childhood Cancer Predisposition
NCT03001349	EARLY_PHASE1	TERMINATED	68Ga-DOTA-TOC PET/CT in Imaging Participants With Neuroendocrine Tumors
NCT01793168	Not specified	RECRUITING	Rare Disease Patient Registry & Natural History Study - Coordination of Rare Diseases at Sanford
NCT01794676	Not specified	COMPLETED	Genetic Evaluation of Families With Endocrine Cancers
NCT03043508	Not specified	UNKNOWN	Overall and Disease Specific Survival in Patients With Confirmed MEN1 With or Without PNET (Pancreatic Neuroendocrine Tumors)
NCT03966612	Not specified	RECRUITING	Study and Monitoring of Multiple Endocrine Neoplasia Type 1
NCT05037461	Not specified	RECRUITING	Precision Radiotherapy Using MR-linac for Pancreatic Neuroendocrine Tumours in MEN1 Patients
NCT05061784	Not specified	COMPLETED	Routine Transcervical Thymectomy in MEN-1 Patients
NCT05554744	Not specified	UNKNOWN	EUS-FNI for MEN1-related Pancreatic Neuroendocrine Tumors
NCT06523582	Not specified	RECRUITING	Genetic Bases of Neuroendocrine Neoplasms in Mexican Patients
NCT06790251	Not specified	NOT_YET_RECRUITING	Institution of an Italian Multicenter Database of Patients With Multiple Endocrine Neoplasia Type 1 (MENNET1 Database)
NCT07272187	Not specified	RECRUITING	Endoscopic Ultrasound-guided Radiofrequency Ablation for Upper Gastrointestinal Tract Lesions
NCT00001595	Not specified	RECRUITING	An Investigation of Pituitary Tumors and Related Hypothalmic Disorders
NCT00461188	Not specified	RECRUITING	Genetics of Endocrine Tumours - Familial Isolated Pituitary Adenoma - FIPA
NCT01775332	Not specified	UNKNOWN	Interdisciplinary Pituitary Disorders Centre of Excellence: Assessment of Patient Education Tools
NCT01369953	Not specified	COMPLETED	Informed Consent for Whole Genome Sequencing: Ideals and Norms Referenced by Early Participants
NCT00001496	Not specified	COMPLETED	Establishment of Normal Breast Epithelial Cell Lines From Patients at High Risk for Breast Cancer