SPIN1

gene
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Also known as TDRD24

Summary

SPIN1 (spindlin 1, HGNC:11243) is a protein-coding gene on chromosome 9q22.1, encoding Spindlin-1 (Q9Y657). Chromatin reader that specifically recognizes and binds histone H3 both trimethylated at ‘Lys-4’ and ‘Lys-9’ (H3K4me3K9me3) and is involved in piRNA-mediated retrotransposon silencing during spermatogenesis.

Enables histone reader activity and methylated histone binding activity. Involved in positive regulation of DNA-templated transcription; positive regulation of Wnt signaling pathway; and rRNA transcription. Located in cytosol and nucleus.

Source: NCBI Gene 10927 — RefSeq curated summary.

At a glance

  • GWAS associations: 4
  • Clinical variants (ClinVar): 22 total
  • Druggable target: yes
  • MANE Select transcript: NM_006717

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:11243
Approved symbolSPIN1
Namespindlin 1
Location9q22.1
Locus typegene with protein product
StatusApproved
AliasesTDRD24
Ensembl geneENSG00000106723
Ensembl biotypeprotein_coding
OMIM609936
Entrez10927

Gene structure

Transcript identifiers

Ensembl transcripts: 78 — 73 protein_coding, 5 protein_coding_CDS_not_defined

ENST00000375859, ENST00000462844, ENST00000469017, ENST00000483785, ENST00000485565, ENST00000485804, ENST00000853460, ENST00000853461, ENST00000853462, ENST00000853463, ENST00000853464, ENST00000853465, ENST00000853466, ENST00000853467, ENST00000853468, ENST00000853469, ENST00000853470, ENST00000853471, ENST00000853472, ENST00000853473, ENST00000853474, ENST00000853475, ENST00000853476, ENST00000853477, ENST00000853478, ENST00000853479, ENST00000853480, ENST00000853481, ENST00000853482, ENST00000853483, ENST00000853484, ENST00000853485, ENST00000853486, ENST00000853487, ENST00000853488, ENST00000853489, ENST00000853490, ENST00000853491, ENST00000853492, ENST00000853493, ENST00000853494, ENST00000853495, ENST00000853496, ENST00000853497, ENST00000853498, ENST00000853499, ENST00000853500, ENST00000853501, ENST00000853502, ENST00000853503, ENST00000928841, ENST00000928842, ENST00000928843, ENST00000928844, ENST00000928845, ENST00000928846, ENST00000928847, ENST00000928848, ENST00000928849, ENST00000928850, ENST00000928851, ENST00000928852, ENST00000928853, ENST00000960823, ENST00000960824, ENST00000960825, ENST00000960826, ENST00000960827, ENST00000960828, ENST00000960829, ENST00000960830, ENST00000960831, ENST00000960832, ENST00000960833, ENST00000960834, ENST00000960835, ENST00000960836, ENST00000960837

RefSeq mRNA: 1 — MANE Select: NM_006717 NM_006717

CCDS: CCDS43843

Canonical transcript exons

ENST00000375859 — 6 exons

ExonStartEnd
ENSE000014685988847507888478694
ENSE000018764008838844488388538
ENSE000034773978846837288468605
ENSE000035925628846249688462749
ENSE000036428768842638288426591
ENSE000036792198844894188448989

Expression profiles

Bgee: expression breadth ubiquitous, 279 present calls, max score 99.14.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 25.4676 / max 330.1331, expressed in 1806 samples.

FANTOM5 promoters (8 alternative TSS)

Promoter IDTPM avgSamples expressed
9725618.39741783
972552.84881156
972571.3093739
972581.0606614
972540.7660369
972530.7267414
972590.212880
972660.146028

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
postcentral gyrusUBERON:000258199.14gold quality
caput epididymisUBERON:000435899.06gold quality
parietal lobeUBERON:000187298.93gold quality
corpus epididymisUBERON:000435998.93gold quality
cortical plateUBERON:000534398.62gold quality
superior vestibular nucleusUBERON:000722798.58gold quality
middle temporal gyrusUBERON:000277198.56gold quality
entorhinal cortexUBERON:000272898.42gold quality
Brodmann (1909) area 23UBERON:001355498.31gold quality
seminal vesicleUBERON:000099898.28gold quality
renal medullaUBERON:000036298.22gold quality
superior frontal gyrusUBERON:000266198.20gold quality
ponsUBERON:000098898.19gold quality
lateral nuclear group of thalamusUBERON:000273698.15gold quality
trigeminal ganglionUBERON:000167598.14gold quality
subthalamic nucleusUBERON:000190698.10gold quality
urethraUBERON:000005798.08gold quality
lateral globus pallidusUBERON:000247698.07gold quality
cauda epididymisUBERON:000436098.06gold quality
ganglionic eminenceUBERON:000402398.04gold quality
oocyteCL:000002398.02gold quality
secondary oocyteCL:000065598.01gold quality
globus pallidusUBERON:000187597.93gold quality
mammary ductUBERON:000176597.92gold quality
medial globus pallidusUBERON:000247797.91gold quality
endometriumUBERON:000129597.87gold quality
parietal pleuraUBERON:000240097.84gold quality
visceral pleuraUBERON:000240197.74gold quality
dorsal root ganglionUBERON:000004497.55gold quality
cerebellar vermisUBERON:000472097.48gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3yes9.24

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

240 targeting SPIN1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3163100.0077.238605
HSA-MIR-6867-5P100.0082.213464
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-8485100.0077.574731
HSA-MIR-3646100.0073.565283
HSA-MIR-656-3P100.0072.152788
HSA-MIR-340-5P100.0072.504437
HSA-MIR-190A-3P100.0080.355520
HSA-MIR-5692A100.0074.406850
HSA-LET-7A-3P100.0074.033932
HSA-LET-7B-3P100.0074.083913
HSA-LET-7F-1-3P100.0074.023928
HSA-MIR-98-3P100.0074.083907
HSA-MIR-548AW99.9972.573559
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-4789-3P99.9970.752484
HSA-MIR-6759-5P99.9966.54785
HSA-MIR-371B-5P99.9975.344759
HSA-MIR-366299.9973.825684
HSA-MIR-33A-5P99.9968.621055
HSA-MIR-33B-5P99.9968.581062
HSA-MIR-513B-5P99.9969.962150
HSA-MIR-428299.9975.366408
HSA-MIR-10401-5P99.9965.79948
HSA-MIR-3692-3P99.9870.272139
HSA-MIR-4789-5P99.9870.762721
HSA-MIR-373-5P99.9875.364753
HSA-MIR-616-5P99.9875.584775
HSA-MIR-56899.9869.862084
HSA-MIR-23B-5P99.9866.07587

Literature-anchored findings (GeneRIF, showing 30)

  • spindlin1 gene may contribute to tumorigenesis (PMID:16098913)
  • recombinant human spindlin1 has been overexpressed in Escherichia coli BL21, purified and crystallized using the hanging-drop vapour-diffusion method (PMID:16472086)
  • analysis of human spindlin1 tudor-like domains for cell cycle regulation (PMID:17082182)
  • SPINDLIN1 is an important gene for mammalian mitotic chromosome functions, and disrupted regulation results in abnormal cell division, a mechanism that may be involved in tumorigenesis (PMID:18201843)
  • Excess spindlin1 protein may be detrimental for spindle microtubule organization, chromosomal stability and can potentially contribute to the development of cancer. (PMID:18543248)
  • Spindlin1 localizes to the active ribosomal DNA (rDNA) repeats, and Spindlin1 facilitates the expression of ribosomal RNA genes. (PMID:21960006)
  • SPINDLIN1, which may be a novel substrate of the Aurora-A kinase, promotes cancer cell growth through WNT/TCF-4 signaling activation. (PMID:22258766)
  • the histone sequence is recognized in a distinct manner involving the amino terminus and a pair of arginine residues of histone H3, and disruption of the binding impaired stimulation of pre-RNA expression by Spindlin1 (PMID:23077255)
  • Spindlin1 activates Wnt/beta-catenin signaling downstream from protein arginine methyltransferase 2 (PRMT2) and the MLL complex, which together are capable of generating a specific H3 “K4me3-R8me2a” pattern. (PMID:24589551)
  • High SPIN1 expression is associated with liposarcoma. (PMID:25749382)
  • These data indicate that miR-489 could reverse the chemoresistance of breast cancer via the PI3K-Akt pathway by targeting SPIN1. (PMID:27171498)
  • In triple negative breast cancer (TNBC) cells the simultaneous miR-29b-1-5p down regulation and SPIN1 up-regulation can potentially be associated with TNBC malignancy. (PMID:28423652)
  • miR-489 loss facilitates malignant phenotype of glioma cells probably via SPIN1-mediated PI3K/AKT pathway. (PMID:28666210)
  • identified SPIN.DOC as a transcriptional repressor that binds SPIN1 and masks its ability to engage the H3-Lys-4 trimethylation activation mark (PMID:29061846)
  • we describe the first example of a histone code reader controlling SkM development in mice, which hints at Spin1 as a potential player in human SkM disease. (PMID:29168801)
  • miR-1271 can suppress breast cancer cell proliferation and progression by targeting SPIN1 expression (PMID:29771421)
  • Results identified a nucleolar localization signal in the N-terminal region of spindlin 1 (SPIN1) that is essential for its enrichment and function in the nucleolus. (PMID:30249398)
  • Data show that spindlin-1 binds methylated arginine R23 of histone H4 (H4), suggsting the function of Spindlin-1. (PMID:30381828)
  • SPINDOC Interacts with SPIN1 in DNA independent manner. SPINDOC regulates expression and chromatin loading of SPIN1. (PMID:30803761)
  • LINC00473/miR-374a-5p regulates esophageal squamous cell carcinoma via targeting SPIN1 to weaken the effect of radiotherapy. (PMID:31017716)
  • SPIN1 triggers abnormal lipid metabolism and enhances tumor growth in liver cancer. (PMID:31790762)
  • E2F1-activated SPIN1 promotes tumor growth via a MDM2-p21-E2F1 feedback loop in gastric cancer. (PMID:32767629)
  • Circ_0086720 knockdown strengthens the radiosensitivity of non-small cell lung cancer via mediating the miR-375/SPIN1 axis. (PMID:32940043)
  • Long noncoding RNA PSMA3AS1 functions as a microRNA4093p sponge to promote the progression of nonsmall cell lung carcinoma by targeting spindlin 1. (PMID:32945481)
  • Structure-Based Design, Docking and Binding Free Energy Calculations of A366 Derivatives as Spindlin1 Inhibitors. (PMID:34072837)
  • The microRNA-381(miR-381)/Spindlin1(SPIN1) axis contributes to cell proliferation and invasion of colorectal cancer cells by regulating the Wnt/beta-catenin pathway. (PMID:34753384)
  • Recognition of Dimethylarginine Analogues by Tandem Tudor Domain Protein Spindlin1. (PMID:35164245)
  • Epigenetic Control of Cancer Cell Proliferation and Cell Cycle Progression by HNRNPK via Promoting Exon 4 Inclusion of Histone Code Reader SPIN1. (PMID:36736887)
  • Molecular Basis for SPINDOC-Spindlin1 Engagement and Its Role in Transcriptional Attenuation. (PMID:37977297)
  • SPIN1 facilitates chemoresistance and HR repair by promoting Tip60 binding to H3K9me3. (PMID:39090319)

Cross-species orthologs

6 orthologs

OrganismSymbolGene ID
danio_reriospinbENSDARG00000035697
danio_reriospinaENSDARG00000058949
mus_musculusSpin1ENSMUSG00000021395
rattus_norvegicusSpin1ENSRNOG00000031378
rattus_norvegicusSpin1ENSRNOG00000064787
rattus_norvegicusENSRNOG00000089199

Paralogs (4): SPIN2A (ENSG00000147059), SPIN4 (ENSG00000186767), SPIN2B (ENSG00000186787), SPIN3 (ENSG00000204271)

Protein

Protein identifiers

Spindlin-1Q9Y657 (reviewed: Q9Y657)

Alternative names: Ovarian cancer-related protein, Spindlin1

All UniProt accessions (1): Q9Y657

UniProt curated annotations — full annotation on UniProt →

Function. Chromatin reader that specifically recognizes and binds histone H3 both trimethylated at ‘Lys-4’ and ‘Lys-9’ (H3K4me3K9me3) and is involved in piRNA-mediated retrotransposon silencing during spermatogenesis. Plays a key role in the initiation of the PIWIL4-piRNA pathway, a pathway that directs transposon DNA methylation and silencing in the male embryonic germ cells, by promoting recruitment of DNA methylation machinery to transposons: binds young, but not old, LINE1 transposons, which are specifically marked with H3K4me3K9me3, and promotes the recruitment of PIWIL4 and SPOCD1 to transposons, leading to piRNA-directed DNA methylation. Also recognizes and binds histone H3 both trimethylated at ‘Lys-4’ and asymmetrically dimethylated at ‘Arg-8’ (H3K4me3 and H3R8me2a) and acts as an activator of Wnt signaling pathway downstream of PRMT2. In case of cancer, promotes cell cancer proliferation via activation of the Wnt signaling pathway. Overexpression induces metaphase arrest and chromosomal instability. Localizes to active rDNA loci and promotes the expression of rRNA genes. May play a role in cell-cycle regulation during the transition from gamete to embryo. Involved in oocyte meiotic resumption, a process that takes place before ovulation to resume meiosis of oocytes blocked in prophase I: may act by regulating maternal transcripts to control meiotic resumption.

Subunit / interactions. Homodimer; may form higher-order oligomers. Interacts with TCF7L2/TCF4; the interaction is direct. Interacts with HABP4 and SERBP1. Interacts with SPINDOC; SPINDOC stabilizes SPIN1 and enhances its association with bivalent H3K4me3K9me3 mark. Interacts with SPOCD1; promoting recruitment of PIWIL4 and SPOCD1 to transposons.

Subcellular location. Nucleus. Nucleolus.

Tissue specificity. Highly expressed in ovarian cancer tissues.

Post-translational modifications. Phosphorylated during oocyte meiotic maturation.

Domain organisation. The 3 tudor-like domains (also named Spin/Ssty repeats) specifically recognize and bind methylated histones. H3K4me3 and H3R8me2a are recognized by tudor-like domains 2 and 1, respectively.

Similarity. Belongs to the SPIN/STSY family.

RefSeq proteins (1): NP_006708* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR003671SPIN/SstyFamily
IPR042567SPIN/Ssty_sfHomologous_superfamily

Pfam: PF02513

UniProt features (59 total): strand 19, mutagenesis site 14, region of interest 7, modified residue 4, site 3, cross-link 3, helix 3, turn 2, chain 1, sequence variant 1, sequence conflict 1, compositionally biased region 1

Structure

Experimental structures (PDB)

20 structures.

PDBMethodResolution (Å)
7OCBX-RAY DIFFRACTION1.42
6I8YX-RAY DIFFRACTION1.52
6I8LX-RAY DIFFRACTION1.58
6QPLX-RAY DIFFRACTION1.6
7CNAX-RAY DIFFRACTION1.6
4MZGX-RAY DIFFRACTION1.7
6I8BX-RAY DIFFRACTION1.76
8GTXX-RAY DIFFRACTION1.8
9T2ZX-RAY DIFFRACTION1.87
4H75X-RAY DIFFRACTION2.1
4MZFX-RAY DIFFRACTION2.1
2NS2X-RAY DIFFRACTION2.2
4MZHX-RAY DIFFRACTION2.2
5JSJX-RAY DIFFRACTION2.35
5JSGX-RAY DIFFRACTION2.5
7E9MX-RAY DIFFRACTION2.5
7EA1X-RAY DIFFRACTION2.7
7BQZX-RAY DIFFRACTION3.1
5Y5WX-RAY DIFFRACTION3.3
7BU9X-RAY DIFFRACTION3.5

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9Y657-F182.140.67

Functional residue map

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

Catalytic / active sites (3): 180 (histone h3k4me3 and h3r8me2a binding); 184 (histone h3k4me3 and h3r8me2a binding); 173 (histone h3k4me3 and h3r8me2a binding)

Post-translational modifications (7): 44, 109, 124, 199, 7, 28, 44

Mutagenesis-validated functional residues (14):

PositionPhenotype
62decreased binding to histone h3 trimethylated at both ’lys-4’ and ’lys-9’ (h3k4me3k9me3).
72impaired binding to histone h3k4me3 and h3r8me2a and impaired ability to activate the wnt signaling pathway. ecreased bi
91decreased binding to histone h3 trimethylated at both ’lys-4’ and ’lys-9’ (h3k4me3k9me3).
98decreased binding to histone h3 trimethylated at both ’lys-4’ and ’lys-9’ (h3k4me3k9me3).
98impaired binding to histone h3k4me3 and h3r8me2a and impaired ability to activate the wnt signaling pathway.
109impaired phosphorylation.
124impaired phosphorylation.
141impaired binding to histone h3k4me3 and h3r8me2a and impaired ability to activate the wnt signaling pathway. impaired ab
142impaired binding to histone h3k4me3 and h3r8me2a.
170impaired binding to histone h3k4me3 and h3r8me2a and impaired ability to activate the wnt signaling pathway. impaired ab
177impaired binding to histone h3k4me3 and h3r8me2a.
184impaired binding to histone h3k4me3 and h3r8me2a.
189impaired binding to histone h3k4me3.
251impaired binding to histone h3k4me3 and h3r8me2a and impaired ability to activate the wnt signaling pathway.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 242 (showing top): TTTGTAG_MIR520D, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, MCBRYAN_PUBERTAL_TGFB1_TARGETS_UP, GOBP_REGULATION_OF_WNT_SIGNALING_PATHWAY, GOBP_RRNA_TRANSCRIPTION, STARK_HYPPOCAMPUS_22Q11_DELETION_UP, MARTINEZ_RB1_TARGETS_UP, GOBP_NEGATIVE_REGULATION_OF_GENE_EXPRESSION_EPIGENETIC, GOBP_DNA_METHYLATION_DEPENDENT_CONSTITUTIVE_HETEROCHROMATIN_FORMATION, CREIGHTON_ENDOCRINE_THERAPY_RESISTANCE_1, GOBP_PROTEIN_LOCALIZATION_TO_CHROMATIN, GOBP_PROTEIN_LOCALIZATION_TO_CHROMOSOME, MCBRYAN_PUBERTAL_BREAST_5_6WK_UP, DODD_NASOPHARYNGEAL_CARCINOMA_UP

GO Biological Process (10): regulation of DNA-templated transcription (GO:0006355), gamete generation (GO:0007276), rRNA transcription (GO:0009303), Wnt signaling pathway (GO:0016055), positive regulation of Wnt signaling pathway (GO:0030177), positive regulation of DNA-templated transcription (GO:0045893), meiotic cell cycle (GO:0051321), protein localization to chromatin (GO:0071168), transposable element silencing by piRNA-mediated DNA methylation (GO:0141196), chromatin organization (GO:0006325)

GO Molecular Function (3): histone H3K4me3 reader activity (GO:0140002), histone reader activity (GO:0140566), protein binding (GO:0005515)

GO Cellular Component (7): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), spindle (GO:0005819), cytosol (GO:0005829), nuclear membrane (GO:0031965)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
DNA-templated transcription3
cellular anatomical structure3
sexual reproduction2
nuclear lumen2
intracellular membraneless organelle2
regulation of gene expression1
regulation of RNA biosynthetic process1
multicellular organismal reproductive process1
rRNA metabolic process1
cell surface receptor signaling pathway1
positive regulation of signal transduction1
Wnt signaling pathway1
regulation of Wnt signaling pathway1
regulation of DNA-templated transcription1
positive regulation of RNA biosynthetic process1
cell cycle1
reproductive process1
meiotic nuclear division1
protein localization to chromosome1
transposable element silencing by heterochromatin formation1
gene silencing by piRNA-directed DNA methylation1
cellular component organization1
histone H3 reader activity1
nucleosome1
histone binding1
chromatin-protein adaptor activity1
binding1
chromosome1
intracellular membrane-bounded organelle1
microtubule cytoskeleton1
cytoplasm1
nucleus1
nuclear envelope1
organelle membrane1

Protein interactions and networks

STRING

536 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
SPIN1SPINDOCQ9BUA3666
SPIN1H3-3AP06351620
SPIN1H3C1P02295619
SPIN1H3-5Q6NXT2618
SPIN1H3-7Q5TEC6617
SPIN1H3C14Q71DI3616
SPIN1H3-4Q16695616
SPIN1CPEB1Q9BZB8497
SPIN1IL3P08700496
SPIN1SETDB1Q15047491
SPIN1SGF29Q96ES7467
SPIN1WDR5P61964452
SPIN1TAF3Q5VWG9426
SPIN1KAT7O95251413
SPIN1PHF23Q9BUL5410

IntAct

56 interactions, top by confidence:

ABTypeScore
SPIN1psi-mi:“MI:0407”(direct interaction)0.650
repEIF4E2psi-mi:“MI:0914”(association)0.640
SPIN1SPINDOCpsi-mi:“MI:0914”(association)0.640
SPIN1psi-mi:“MI:0915”(physical association)0.560
SPINDOCSPIN3psi-mi:“MI:0914”(association)0.560
ZNF324BZNF316psi-mi:“MI:0914”(association)0.530
SPIN2BWDHD1psi-mi:“MI:0914”(association)0.530
SPIN1PAX3psi-mi:“MI:0914”(association)0.530
CUEDC1TOM1psi-mi:“MI:0914”(association)0.530
ZNF324BZNF324psi-mi:“MI:0914”(association)0.530
HSPB1SPIN1psi-mi:“MI:0915”(physical association)0.510
SPIN1HSPB1psi-mi:“MI:0915”(physical association)0.510
HMGB1SPIN1psi-mi:“MI:0915”(physical association)0.370
SPIN1PRMT6psi-mi:“MI:0915”(physical association)0.370
ARRB1psi-mi:“MI:0914”(association)0.350
ARRB2psi-mi:“MI:0914”(association)0.350
HSD17B10HMGB1P1psi-mi:“MI:0914”(association)0.350
SOD1NPEPPSL1psi-mi:“MI:0914”(association)0.350
VDAC1SNRPGP15psi-mi:“MI:0914”(association)0.350
AGO3PRMT5psi-mi:“MI:0914”(association)0.350

BioGRID (144): SPIN1 (Affinity Capture-MS), SPIN4 (Affinity Capture-MS), SUPT16H (Affinity Capture-MS), BCLAF1 (Affinity Capture-MS), THRAP3 (Affinity Capture-MS), CGGBP1 (Affinity Capture-MS), SSRP1 (Affinity Capture-MS), YRDC (Affinity Capture-MS), C11orf84 (Affinity Capture-MS), MCM2 (Affinity Capture-MS), ZGPAT (Affinity Capture-MS), SF3A3 (Affinity Capture-MS), SCNM1 (Affinity Capture-MS), TOPORS (Affinity Capture-MS), PAX3 (Affinity Capture-MS)

ESM2 similar proteins: A0A8I5ZNK2, A2A432, A9X1D0, B0VX69, B1MTJ4, B2KI88, B5FW36, B7ZUF3, C1FXW2, D2XV59, E1C1R4, F4JL28, O00178, O08582, O70133, O75688, O88506, O95747, P11029, P23727, P26450, P27986, P40692, P60762, Q13085, Q13330, Q4V8J7, Q503N9, Q58DC5, Q5R495, Q5R685, Q5R8Q7, Q5R997, Q5ZML9, Q61142, Q62599, Q63787, Q6P9R2, Q863I2, Q86TU7

Diamond homologs: P13675, Q2KI39, Q4V8J7, Q56A73, Q5JUX0, Q5R997, Q5RA80, Q5RAW7, Q61142, Q6NVE3, Q8K1L2, Q90WG1, Q90WG2, Q99865, Q9BPZ2, Q9Y657

SIGNOR signaling

2 interactions.

AEffectBMechanism
AURKA“up-regulates activity”SPIN1phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance10
Likely benign0
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

2268 predictions. Top by Δscore:

VariantEffectΔscore
9:88388535:GCAG:Gdonor_gain1.0000
9:88388536:CAG:Cdonor_loss1.0000
9:88388537:AG:Adonor_loss1.0000
9:88388538:GG:Gdonor_loss1.0000
9:88388539:GT:Gdonor_loss1.0000
9:88388540:T:Adonor_loss1.0000
9:88426379:CAGAG:Cacceptor_loss1.0000
9:88426380:A:AGacceptor_gain1.0000
9:88426380:AGAGT:Aacceptor_gain1.0000
9:88426381:G:GCacceptor_loss1.0000
9:88426381:G:GGacceptor_gain1.0000
9:88426381:GA:Gacceptor_gain1.0000
9:88426381:GAGT:Gacceptor_gain1.0000
9:88426381:GAGTG:Gacceptor_gain1.0000
9:88426590:AGG:Adonor_loss1.0000
9:88426592:G:GAdonor_loss1.0000
9:88426593:T:Adonor_loss1.0000
9:88433681:A:AGacceptor_gain1.0000
9:88433682:A:Gacceptor_gain1.0000
9:88448935:TTACA:Tacceptor_loss1.0000
9:88448936:TACA:Tacceptor_loss1.0000
9:88448937:ACAGG:Aacceptor_loss1.0000
9:88448938:CA:Cacceptor_loss1.0000
9:88448939:A:AGacceptor_gain1.0000
9:88448939:A:Gacceptor_loss1.0000
9:88448939:AG:Aacceptor_gain1.0000
9:88448940:G:GAacceptor_gain1.0000
9:88448940:GG:Gacceptor_gain1.0000
9:88448940:GGC:Gacceptor_gain1.0000
9:88448940:GGCC:Gacceptor_gain1.0000

AlphaMissense

1736 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
9:88462567:T:AI58N1.000
9:88462578:T:AW62R1.000
9:88462578:T:CW62R1.000
9:88462580:G:CW62C1.000
9:88462580:G:TW62C1.000
9:88462608:T:AW72R1.000
9:88462608:T:CW72R1.000
9:88462609:G:CW72S1.000
9:88462610:G:CW72C1.000
9:88462610:G:TW72C1.000
9:88462614:G:AG74R1.000
9:88462614:G:CG74R1.000
9:88462615:G:AG74E1.000
9:88462615:G:TG74V1.000
9:88462621:T:AV76D1.000
9:88462624:T:AL77Q1.000
9:88462624:T:CL77P1.000
9:88462651:T:CL86S1.000
9:88462657:T:CL88P1.000
9:88462660:T:AI89K1.000
9:88462662:A:GK90E1.000
9:88462663:A:TK90I1.000
9:88462664:A:CK90N1.000
9:88462664:A:TK90N1.000
9:88462665:T:CY91H1.000
9:88462677:G:CD95H1.000
9:88462677:G:TD95Y1.000
9:88462678:A:GD95G1.000
9:88462678:A:TD95V1.000
9:88462681:G:AC96Y1.000

dbSNP variants (sampled 300 via entrez): RS1000076624 (9:88428572 G>A), RS1000084295 (9:88400968 G>A,C), RS1000090219 (9:88393604 T>C), RS1000139185 (9:88459376 T>A,C,G), RS1000163793 (9:88473028 C>G), RS1000206047 (9:88468204 G>A), RS1000213358 (9:88459673 C>T), RS1000215960 (9:88403989 C>T), RS1000232687 (9:88432652 T>G), RS1000339664 (9:88390931 A>G,T), RS1000361098 (9:88433873 A>G), RS1000367905 (9:88389429 C>T), RS1000372594 (9:88456892 A>G), RS1000381651 (9:88442396 T>A,C), RS1000417894 (9:88428293 A>G)

Disease associations

OMIM: gene MIM:609936 | 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):

StudyTraitp-value
GCST000175_1Height9.000000e-07
GCST000817_172Height9.000000e-13
GCST006192_44Systolic blood pressure x smoking status (ever vs never) interaction (2df test)4.000000e-09
GCST008839_235Height1.000000e-10

EFO canonical traits (2, from GWAS)

EFO IDTrait name
EFO:0006335systolic blood pressure
EFO:0006527smoking status measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4523509 (SINGLE PROTEIN)

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — Methyllysine reader proteins

Most potent curated ligand interactions (2 total), top 2:

LigandActionAffinityParameter
MS8535Binding7.52pKd
MS31Binding7.04pKd

ChEMBL bioactivities

75 potent at pChembl≥5 of 76 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.18Kd6.6nMCHEMBL4573889
8.00Kd9.9nMCHEMBL4451634
8.00Kd10.1nMCHEMBL4570122
7.81Kd15.4nMCHEMBL4528213
7.75Kd18nMCHEMBL5575917
7.52Kd30nMCHEMBL5594627
7.48IC5033nMCHEMBL4451634
7.47Kd34nMCHEMBL5572612
7.35Kd45nMCHEMBL5575071
7.32IC5048nMCHEMBL4573889
7.29Kd51nMCHEMBL5570983
7.26Kd55nMCHEMBL4451634
7.23IC5059nMCHEMBL4570122
7.22Kd60nMCHEMBL4577068
7.17Kd67nMCHEMBL4573889
7.14Kd72nMCHEMBL4570122
7.14IC5072nMCHEMBL3109630
7.11IC5077nMCHEMBL4552020
7.06Kd88nMCHEMBL5583678
7.04Kd91nMCHEMBL4552020
7.04Kd92nMCHEMBL5564247
7.03Kd94nMCHEMBL4528213
6.96Kd110nMCHEMBL3109630
6.95Kd111.1nMCHEMBL4451634
6.94Kd114nMCHEMBL5572650
6.82IC50152nMCHEMBL4577068
6.79Kd164nMCHEMBL5568957
6.75Kd180nMCHEMBL3109630
6.73IC50186nMCHEMBL3109630
6.73IC50187nMCHEMBL5570983
6.71IC50197nMCHEMBL5572612
6.70IC50200nMCHEMBL5575071
6.70IC50202nMCHEMBL5594627
6.69IC50203nMCHEMBL5575917
6.68IC50207nMCHEMBL3109630
6.67IC50214nMCHEMBL5564247
6.67IC50215nMCHEMBL5583678
6.61IC50243nMCHEMBL4552020
6.57EC50270nMCHEMBL4451634
6.51IC50312nMCHEMBL5572650
6.49IC50326nMCHEMBL5590823
6.47IC50340nMCHEMBL4591023
6.47IC50338nMCHEMBL4588285
6.46IC50348nMCHEMBL5568957
6.44IC50360nMCHEMBL4528213
6.41IC50390nMCHEMBL4476309
6.41Kd393nMCHEMBL3109630
6.41Kd390nMCHEMBL4588285
6.40Kd400nMCHEMBL4577068
6.22IC50600nMCHEMBL4518756

PubChem BioAssay actives

75 with measured affinity, of 94 total; 38 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
3-[4-[[2-[3-[2-amino-5-(cyclopropylmethoxy)-3,3-dimethylindol-6-yl]oxypropyl]-1,3-dihydroisoindol-5-yl]oxymethyl]triazol-1-yl]-1-[4-(2-pyrrolidin-1-ylethyl)piperidin-1-yl]propan-1-one1526499: Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0066uM
2-[4-[2-[[2-[3-[2-amino-5-(cyclopropylmethoxy)-3,3-dimethylindol-6-yl]oxypropyl]-1,3-dihydroisoindol-5-yl]oxy]ethyl]triazol-1-yl]-1-[4-(2-pyrrolidin-1-ylethyl)piperidin-1-yl]ethanone1526499: Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0099uM
3-[4-[2-[[2-[3-[2-amino-5-(cyclopropylmethoxy)-3,3-dimethylindol-6-yl]oxypropyl]-1,3-dihydroisoindol-5-yl]oxy]ethyl]triazol-1-yl]-1-[4-(2-pyrrolidin-1-ylethyl)piperidin-1-yl]propan-1-one1526499: Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0101uM
5-(cyclopropylmethoxy)-6-[3-(1,3-dihydroisoindol-2-yl)propoxy]-3,3-dimethylindol-2-amine1526499: Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0154uM
7-[3-(1,3-dihydroisoindol-2-yl)propoxy]-2-N-[2-(dimethylamino)ethyl]-6-methoxy-4-N-(1-propan-2-ylpiperidin-4-yl)quinazoline-2,4-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0180uM
N-[7-[3-(1,3-dihydroisoindol-2-yl)propoxy]-6-methoxy-4-pyrrolidin-1-ylquinazolin-2-yl]-N’,N’-dimethylethane-1,2-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0300uM
7-[3-(1,3-dihydroisoindol-2-yl)propoxy]-2-N-[3-(dimethylamino)propyl]-6-methoxy-4-N-(1-propan-2-ylpiperidin-4-yl)quinoline-2,4-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0340uM
2-N-[2-(dimethylamino)ethyl]-6-methoxy-4-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazoline-2,4-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0450uM
7-[3-(1,3-dihydroisoindol-2-yl)propoxy]-6-methoxy-4-N-(1-propan-2-ylpiperidin-4-yl)-2-N-(2-pyrrolidin-1-ylethyl)quinoline-2,4-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0510uM
2-[4-[[2-[3-[2-amino-5-(cyclopropylmethoxy)-3,3-dimethylindol-6-yl]oxypropyl]-1,3-dihydroisoindol-5-yl]oxymethyl]triazol-1-yl]-1-[4-(2-pyrrolidin-1-ylethyl)piperidin-1-yl]ethanone1526499: Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0600uM
5’-methoxy-6’-(3-pyrrolidin-1-ylpropoxy)spiro[cyclobutane-1,3’-indole]-2’-amine1578933: Inhibition of biotin-H3(1-23)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 90 mins by AlphaLISA assayic500.0720uM
[3-(aminomethyl)-5-[3-(1,3-dihydroisoindol-2-yl)propoxy]-4-methoxyphenyl]methanamine1578933: Inhibition of biotin-H3(1-23)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 90 mins by AlphaLISA assayic500.0770uM
7-[3-(1,3-dihydroisoindol-2-yl)propoxy]-6-methoxy-2-N-[(1-methylpyrrolidin-2-yl)methyl]-4-N-(1-propan-2-ylpiperidin-4-yl)quinoline-2,4-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0880uM
7-[3-(1,3-dihydroisoindol-2-yl)propoxy]-6-methoxy-2-N-(2-piperidin-1-ylethyl)-4-N-(1-propan-2-ylpiperidin-4-yl)quinoline-2,4-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.0920uM
6-methoxy-4-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazoline-2,4-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.1140uM
7-[3-(1,3-dihydroisoindol-2-yl)propoxy]-6-methoxy-2-N-(2-morpholin-4-ylethyl)-4-N-(1-propan-2-ylpiperidin-4-yl)quinoline-2,4-diamine2103405: Binding affinity to human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd0.1640uM
7-[3-(1,3-dihydroisoindol-2-yl)propoxy]-2-N-[2-(dimethylamino)ethyl]-6-methoxy-4-N-(1-propan-2-ylpiperidin-4-yl)quinoline-2,4-diamine2103404: Displacement of FL-H3K4me3 peptide from human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assayic500.3260uM
[3-(aminomethyl)-4-methoxy-5-(3-pyrrolidin-1-ylpropoxy)phenyl]methanamine1578933: Inhibition of biotin-H3(1-23)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 90 mins by AlphaLISA assayic500.3380uM
5’-(cyclopropylmethoxy)-6’-[3-(5-methoxy-1,3-dihydroisoindol-2-yl)propoxy]spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic500.3400uM
5’-(cyclopropylmethoxy)-6’-[3-(1,3-dihydroisoindol-2-yl)propoxy]spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic500.3900uM
5’-methoxy-6’-[3-(5-methoxy-1,3-dihydroisoindol-2-yl)propoxy]spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic500.6000uM
6’-[3-(1,3-dihydroisoindol-2-yl)propoxy]-5’-methoxyspiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic500.6600uM
5’-methoxy-6’-(3-pyrrolidin-1-ylpropoxy)spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic500.7600uM
6-methoxy-4-pyrrolidin-1-yl-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-2-amine2103404: Displacement of FL-H3K4me3 peptide from human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assayic500.8380uM
5’-(cyclopropylmethoxy)-6’-(3-pyrrolidin-1-ylpropoxy)spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic501.1200uM
2-[4-[[2-[4-[2-amino-5-(cyclopropylmethoxy)-3,3-dimethylindol-6-yl]oxybutyl]-1,3-dihydroisoindol-5-yl]oxymethyl]triazol-1-yl]-1-[4-(2-pyrrolidin-1-ylethyl)piperidin-1-yl]ethanone1526499: Binding affinity to recombinant human His-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by isothermal titration calorimetrykd1.3000uM
6-methoxy-4-piperidin-1-yl-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-2-amine2103404: Displacement of FL-H3K4me3 peptide from human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assayic501.3200uM
4-N-cyclohexyl-6-methoxy-4-N-methyl-7-(3-pyrrolidin-1-ylpropoxy)quinazoline-2,4-diamine2103404: Displacement of FL-H3K4me3 peptide from human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assayic501.7400uM
6-methoxy-2-N-methyl-4-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazoline-2,4-diamine2103404: Displacement of FL-H3K4me3 peptide from human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assayic502.0600uM
5’-ethoxy-6’-(3-pyrrolidin-1-ylpropoxy)spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic502.1500uM
[4-[4-(2-pyrrolidin-1-ylethyl)piperidine-1-carbonyl]-3-[4-(pyrrolidin-1-ylmethoxy)anilino]phenyl]-[4-(2-pyrrolidin-1-ylethyl)piperidin-1-yl]methanone1578926: Inhibition of SPIN1 (unknown origin) assessed as dissociation constant by isothermal titration calorimetrykd3.0000uM
2-cyclohexyl-6-methoxy-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine1578933: Inhibition of biotin-H3(1-23)K4me3 binding to recombinant human C-terminal His6-tagged SPIN1 (49 to 262 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 90 mins by AlphaLISA assayic503.2000uM
6-methoxy-4-[(1-propan-2-ylpiperidin-4-yl)amino]-7-(3-pyrrolidin-1-ylpropoxy)-1H-quinazolin-2-one2103404: Displacement of FL-H3K4me3 peptide from human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assayic503.9900uM
5’-(cyclopropylmethoxy)-6’-[4-(1,3-dihydroisoindol-2-yl)butoxy]spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic506.2200uM
5’-methoxy-6’-[3-(4-methoxy-1,3-dihydroisoindol-2-yl)propoxy]spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic506.6500uM
5-(cyclopropylmethoxy)-6-[4-(1,3-dihydroisoindol-2-yl)butoxy]-3,3-dimethylindol-2-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic506.9200uM
6-methoxy-2-N,2-N-dimethyl-4-N-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazoline-2,4-diamine2103404: Displacement of FL-H3K4me3 peptide from human N-terminal His10 tagged SPIN1 (G21 to S262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins by fluorescence polarization assayic507.9700uM
5’-propan-2-yloxy-6’-(3-pyrrolidin-1-ylpropoxy)spiro[cyclopentane-1,3’-indole]-2’-amine1526494: Displacement of trimethylated biotinylated histone H3 peptide from recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins followed by peptide addition and measured after 1 hr by Alphascreen methodic508.9100uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Benzo(a)pyreneaffects methylation, decreases methylation2
Aflatoxin B1increases methylation2
aristolochic acid Idecreases expression1
bisphenol Faffects cotreatment, decreases expression1
TAK-243affects sumoylation1
triphenyl phosphateaffects expression1
alpha-pineneaffects cotreatment, increases oxidation, increases abundance1
bisphenol Aaffects cotreatment, increases methylation1
arseniteaffects binding, decreases reaction1
benzo(e)pyreneincreases methylation1
aflatoxin B2decreases methylation1
methacrylaldehydeincreases abundance, affects cotreatment, increases oxidation1
ICG 001increases expression1
abrinedecreases expression1
3-(2-hydroxy-4-(2-methylnonan-2-yl)phenyl)cyclohexan-1-oldecreases expression1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acidincreases expression1
Fulvestrantaffects cotreatment, increases methylation1
Vorinostatdecreases expression1
Acroleinaffects cotreatment, increases oxidation, increases abundance1
Air Pollutantsincreases abundance, increases oxidation, affects cotreatment1
Dexamethasoneaffects cotreatment, decreases expression1
Endosulfandecreases expression1
Hydrogen Peroxideaffects expression1
Indomethacinaffects cotreatment, decreases expression1
Methapyrileneincreases methylation1
Ozoneincreases oxidation, increases abundance, affects cotreatment1
Rotenoneincreases expression1
Thiramdecreases expression1
Tretinoindecreases expression1
Valproic Acidaffects expression1

ChEMBL screening assays

18 unique, capped per target: 18 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL4323086BindingBinding affinity to recombinant human His-tagged SPIN1 (26 to 262 residues) expressed in Escherichia coli BL21 (DE3) assessed as melting temperature at 20 uM by Sypro orange dye based differential scanning fluorimetryA Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function. — J Med Chem

Clinical trials (associated diseases)

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

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.