CDIPT

Summary

CDIPT (CDP-diacylglycerol–inositol 3-phosphatidyltransferase, HGNC:1769) is a protein-coding gene on chromosome 16p11.2, encoding CDP-diacylglycerol–inositol 3-phosphatidyltransferase (O14735). Catalyzes the biosynthesis of phosphatidylinositol (PtdIns) as well as PtdIns:inositol exchange reaction. It is a selective cancer dependency (DepMap: 83.0% of cell lines).

Phosphatidylinositol breakdown products are ubiquitous second messengers that function downstream of many G protein-coupled receptors and tyrosine kinases regulating cell growth, calcium metabolism, and protein kinase C activity. Two enzymes, CDP-diacylglycerol synthase and phosphatidylinositol synthase, are involved in the biosynthesis of phosphatidylinositol. Phosphatidylinositol synthase, a member of the CDP-alcohol phosphatidyl transferase class-I family, is an integral membrane protein found on the cytoplasmic side of the endoplasmic reticulum and the Golgi apparatus. Several transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 10423 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 35 total — 4 pathogenic, 1 likely-pathogenic
• Druggable target: yes
• Cancer dependency (DepMap): dependent in 83.0% of screened cell lines
• MANE Select transcript: NM_006319

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1769
Approved symbol	CDIPT
Name	CDP-diacylglycerol–inositol 3-phosphatidyltransferase
Location	16p11.2
Locus type	gene with protein product
Status	Approved
Aliases	PIS1, PIS
Ensembl gene	ENSG00000103502
Ensembl biotype	protein_coding
OMIM	605893
Entrez	10423

Gene structure

Transcript identifiers

Ensembl transcripts: 12 — 8 protein_coding, 2 retained_intron, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000219789, ENST00000561555, ENST00000562041, ENST00000563415, ENST00000563893, ENST00000564296, ENST00000566113, ENST00000567459, ENST00000569956, ENST00000570016, ENST00000853345, ENST00000934102

RefSeq mRNA: 3 — MANE Select: NM_006319 NM_001286585, NM_001286586, NM_006319

CCDS: CCDS10657, CCDS67002

Canonical transcript exons

ENST00000219789 — 6 exons

Exon	Start	End
ENSE00000681573	29862586	29862720
ENSE00001231826	29862815	29863226
ENSE00001548141	29858357	29859334
ENSE00003549659	29859442	29859523
ENSE00003610655	29861106	29861259
ENSE00003654788	29860581	29860662

Expression profiles

Bgee: expression breadth ubiquitous, 299 present calls, max score 99.74.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 44.3064 / max 446.2443, expressed in 1823 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
156963	39.6898	1823
156962	1.9483	1288
156959	1.1164	768
156960	0.9363	602
156961	0.5632	359
156958	0.0467	20
156964	0.0057	3

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
parotid gland	UBERON:0001831	99.74	gold quality
endothelial cell	CL:0000115	99.58	gold quality
cervix squamous epithelium	UBERON:0006922	99.41	gold quality
Brodmann (1909) area 23	UBERON:0013554	99.23	gold quality
sperm	CL:0000019	99.07	gold quality
middle temporal gyrus	UBERON:0002771	98.98	gold quality
pancreatic ductal cell	CL:0002079	98.97	gold quality
germinal epithelium of ovary	UBERON:0001304	98.95	gold quality
visceral pleura	UBERON:0002401	98.95	gold quality
parietal pleura	UBERON:0002400	98.81	gold quality
gingival epithelium	UBERON:0001949	98.80	gold quality
cardia of stomach	UBERON:0001162	98.77	gold quality
mammary duct	UBERON:0001765	98.73	gold quality
renal medulla	UBERON:0000362	98.71	gold quality
adult organism	UBERON:0007023	98.69	gold quality
male germ cell	CL:0000015	98.65	gold quality
dorsal root ganglion	UBERON:0000044	98.63	gold quality
gingiva	UBERON:0001828	98.60	gold quality
epithelium of mammary gland	UBERON:0003244	98.59	gold quality
pericardium	UBERON:0002407	98.57	gold quality
pleura	UBERON:0000977	98.50	gold quality
pons	UBERON:0000988	98.49	gold quality
trigeminal ganglion	UBERON:0001675	98.44	gold quality
seminal vesicle	UBERON:0000998	98.38	gold quality
pylorus	UBERON:0001166	98.38	gold quality
urethra	UBERON:0000057	98.37	gold quality
nipple	UBERON:0002030	98.30	gold quality
right hemisphere of cerebellum	UBERON:0014890	98.27	gold quality
choroid plexus epithelium	UBERON:0003911	98.25	gold quality
cerebellar hemisphere	UBERON:0002245	98.19	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	11.33
E-MTAB-7606	no	1128.06

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

29 targeting CDIPT, 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-6755-5P	99.95	65.59	464
HSA-MIR-4697-3P	99.89	67.09	1123
HSA-MIR-4766-5P	99.75	69.23	2662
HSA-MIR-3913-3P	99.74	66.53	938
HSA-MIR-4666A-5P	99.41	69.72	1887
HSA-MIR-940	99.37	66.14	2064
HSA-MIR-6808-5P	99.31	66.23	2150
HSA-MIR-6893-5P	99.31	66.25	2119
HSA-MIR-4685-5P	99.25	65.99	1563
HSA-MIR-6837-5P	99.25	65.47	1632
HSA-MIR-3925-5P	99.21	67.90	1466
HSA-MIR-5190	99.15	67.76	1234
HSA-MIR-4650-3P	99.01	68.39	1062
HSA-MIR-939-3P	98.97	65.07	2347
HSA-MIR-6889-3P	98.84	67.35	1198
HSA-MIR-4477A	98.83	69.75	2952
HSA-MIR-5006-5P	98.79	66.92	1246
HSA-MIR-4755-3P	98.77	65.59	1915
HSA-MIR-6529-3P	98.68	66.76	1020
HSA-MIR-7977	98.65	66.18	2590
HSA-MIR-6792-5P	98.39	68.16	1330
HSA-MIR-3132	97.96	67.91	711
HSA-MIR-3691-3P	97.90	65.97	791
HSA-MIR-197-5P	97.23	68.10	596
HSA-MIR-3649	96.85	64.10	340
HSA-MIR-3059-3P	96.71	67.08	606
HSA-MIR-550B-3P	95.43	67.73	599
HSA-MIR-5684	93.17	64.85	454
HSA-MIR-4258	90.68	62.19	164

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 83.0% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 2)

• AAT Deficiency affects at least 120.5 million carriers and deficient subjects worldwide for the two most prevalent deficiency alleles PIZ. (PMID:16312203)
• Increased CDIPT expression was found to be an early event in oral cancer and a target for smokeless tobacco. (PMID:20426864)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	cdipt	ENSDARG00000070686
mus_musculus	Cdipt	ENSMUSG00000030682
rattus_norvegicus	Cdipt	ENSRNOG00000024144
drosophila_melanogaster	Pis	FBGN0030670
caenorhabditis_elegans		WBGENE00012897

Protein

Protein identifiers

CDP-diacylglycerol–inositol 3-phosphatidyltransferase — O14735 (reviewed: O14735)

Alternative names: Phosphatidylinositol synthase

All UniProt accessions (5): O14735, A8K3L7, B3KY94, H3BTJ7, H3BUR9

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the biosynthesis of phosphatidylinositol (PtdIns) as well as PtdIns:inositol exchange reaction. May thus act to reduce an excessive cellular PtdIns content. The exchange activity is due to the reverse reaction of PtdIns synthase and is dependent on CMP, which is tightly bound to the enzyme.

Subcellular location. Endoplasmic reticulum membrane. Cell membrane.

Tissue specificity. Detected in placenta (at protein level). Widely expressed. Higher expression in adult liver and skeletal muscle, slightly lower levels seen in pancreas, kidney, lung, placenta, brain, heart, leukocyte, colon, small intestine, ovary, testis, prostate, thymus and spleen. In fetus, expressed in kidney, liver, lung and brain.

Activity regulation. Inhibited by PtdIns (product inhibition), phosphatidylinositol phosphate, and nucleoside di- and tri-phosphates.

Cofactor. Catalytic activity is higher with Mg(2+).

Similarity. Belongs to the CDP-alcohol phosphatidyltransferase class-I family.

Isoforms (3)

UniProt ID	Names	Canonical?
O14735-1	1	yes
O14735-2	2
O14735-3	3

RefSeq proteins (3): NP_001273514, NP_001273515, NP_006310* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000462	CDP-OH_P_trans	Family
IPR014387	CDP_diag_ino_3_P_euk	Family
IPR043130	CDP-OH_PTrfase_TM_dom	Homologous_superfamily
IPR048254	CDP_ALCOHOL_P_TRANSF_CS	Conserved_site

Pfam: PF01066

Enzyme classification (BRENDA):

• EC 2.7.8.11 — CDP-diacylglycerol-inositol 3-phosphatidyltransferase (BRENDA: 28 organisms, 71 substrates, 51 inhibitors, 46 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

12 substrates with measured Km, best-characterized 12. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
MYO-INOSITOL	0.015–2.5	23
CDP-DIACYLGLYCEROL	0.0095–0.21	10
2-DEOXY-CDP-DIACYLGLYCEROL	0.029–0.045	2
CDP-DIPALMITIN	0.0193–0.0195	2
CMP	0.022–2.8	2
CDP-1-STEAROYL-2-ARACHIDONOYLGLYCEROL	0.045	1
CDP-1-STEAROYL-2-OLEOYLGLYCEROL	0.03	1
CDP-DIDECANOYL-SN-GLYCEROL	0.06	1
CDP-DIGLYCERIDE	0.17	1
CDP-DIPALMITOYL-SN-GLYCEROL	0.05	1
CDP-DIPALMITOYLGLYCERIDE	1.35	1
CDP-DISTEAROYLGLYCEROL	0.16	1

Catalyzed reactions (Rhea), 1 shown:

• a CDP-1,2-diacyl-sn-glycerol + myo-inositol = a 1,2-diacyl-sn-glycero-3-phospho-(1D-myo-inositol) + CMP + H(+) (RHEA:11580)

UniProt features (30 total): binding site 9, topological domain 7, transmembrane region 6, splice variant 4, chain 1, active site 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O14735-F1	90.02	0.71

Functional residue map

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

Catalytic / active sites (1): 72 (proton acceptor)

Ligand- & substrate-binding residues (9): 47; 47; 50; 51; 55; 61; 68; 68; 72

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-1483226	Synthesis of PI
R-HSA-1430728	Metabolism
R-HSA-1483206	Glycerophospholipid biosynthesis
R-HSA-1483257	Phospholipid metabolism
R-HSA-556833	Metabolism of lipids

MSigDB gene sets: 200 (showing top): GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLINOSITOL_METABOLIC_PROCESS, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, THEILGAARD_NEUTROPHIL_AT_SKIN_WOUND_DN, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, SCIBETTA_KDM5B_TARGETS_UP, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, GOBP_PHOSPHOLIPID_BIOSYNTHETIC_PROCESS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, BLALOCK_ALZHEIMERS_DISEASE_UP, chr16p11, JAZAG_TGFB1_SIGNALING_VIA_SMAD4_UP, MORF_PPP6C, GOBP_GLYCEROLIPID_BIOSYNTHETIC_PROCESS, MORF_PPP2R4

GO Biological Process (4): phosphatidylinositol biosynthetic process (GO:0006661), CDP-diacylglycerol metabolic process (GO:0046341), lipid metabolic process (GO:0006629), phospholipid biosynthetic process (GO:0008654)

GO Molecular Function (9): CDP-diacylglycerol-inositol 3-phosphatidyltransferase activity (GO:0003881), diacylglycerol binding (GO:0019992), manganese ion binding (GO:0030145), carbohydrate binding (GO:0030246), alcohol binding (GO:0043178), protein binding (GO:0005515), transferase activity (GO:0016740), phosphotransferase activity, for other substituted phosphate groups (GO:0016780), metal ion binding (GO:0046872)

GO Cellular Component (5): endoplasmic reticulum membrane (GO:0005789), Golgi apparatus (GO:0005794), plasma membrane (GO:0005886), membrane (GO:0016020), endoplasmic reticulum (GO:0005783)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
Glycerophospholipid biosynthesis	1
Phospholipid metabolism	1
Metabolism of lipids	1
Metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
binding	2
cytoplasm	2
endomembrane system	2
intracellular membrane-bounded organelle	2
biosynthetic process	1
phosphatidylinositol metabolic process	1
glycerophospholipid metabolic process	1
primary metabolic process	1
phospholipid metabolic process	1
lipid biosynthetic process	1
organophosphate biosynthetic process	1
CDP-alcohol phosphatidyltransferase activity	1
lipid binding	1
transition metal ion binding	1
small molecule binding	1
catalytic activity	1
transferase activity, transferring phosphorus-containing groups	1
cation binding	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

2938 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CDIPT	TAMM41	Q96BW9	962
CDIPT	PIM1	P11309	914
CDIPT	SERPINA1	P01009	832
CDIPT	CEPT1	Q9Y6K0	791
CDIPT	ISYNA1	Q9NPH2	724
CDIPT	CDS1	Q92903	716
CDIPT	ASPHD1	Q5U4P2	698
CDIPT	SELENOI	Q9C0D9	690
CDIPT	PGS1	Q32NB8	680
CDIPT	SERPINA3	P01011	679
CDIPT	C16orf54	Q6UWD8	670
CDIPT	CDS2	O95674	665
CDIPT	PEMT	Q9UBM1	643
CDIPT	KCTD13	Q8WZ19	628
CDIPT	PISD	Q9UG56	628

IntAct

264 interactions, top by confidence:

A	B	Type	Score
CDIPT	SDCBP	psi-mi:“MI:0915”(physical association)	0.560
RTN3	CDIPT	psi-mi:“MI:0915”(physical association)	0.560
SDCBP	CDIPT	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	RTN3	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	HSD17B13	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	FCGR2A	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	EVI2B	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	CYB5R3	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	TMX2	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	IER3IP1	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	RNF19B	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	CYB561	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	CGRRF1	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	KIR2DL3	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	GJB1	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	SLC16A7	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	MTIF3	psi-mi:“MI:0915”(physical association)	0.560
CDIPT		psi-mi:“MI:0915”(physical association)	0.560
CDIPT	GPR151	psi-mi:“MI:0915”(physical association)	0.560
CDIPT	JAGN1	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (197): CDIPT (Affinity Capture-MS), CDIPT (Two-hybrid), CDIPT (Two-hybrid), CDIPT (Affinity Capture-MS), CDIPT (Affinity Capture-MS), CDIPT (Affinity Capture-MS), CDIPT (Affinity Capture-MS), SMAP2 (Affinity Capture-MS), YTHDF1 (Affinity Capture-MS), DSCC1 (Affinity Capture-MS), TTC5 (Affinity Capture-MS), UQCC1 (Affinity Capture-MS), CDIPT (Affinity Capture-MS), CDIPT (Affinity Capture-MS), CDIPT (Affinity Capture-MS)

ESM2 similar proteins: A0A077K9K6, A0A1V0QSF1, A1JHN0, A2Z1F5, A8J0J0, B2WAQ3, B8AIW3, E3Q717, O14735, O64886, O82568, O88455, P32378, P70500, Q0D576, Q0DAK7, Q0WUA3, Q10153, Q10252, Q16QL3, Q1ACB3, Q298G6, Q2N2K1, Q2N2K2, Q2N2K3, Q2N2K4, Q499N4, Q5E9J5, Q5N808, Q66JT7, Q69PA8, Q6C0L2, Q6ETL8, Q75F43, Q7XB13, Q7XB14, Q7XR51, Q7YRU6, Q8N2U9, Q8VDP6

Diamond homologs: A1AC64, O14735, O67908, P06197, P0ABF8, P0ABF9, P0ABG0, P70500, Q0T3L5, Q0TGS6, Q10153, Q1RAM8, Q322L9, Q32HD9, Q3IYX7, Q3Z2T6, Q57N57, Q59RA2, Q5PI18, Q7CQB9, Q83R47, Q8D2N9, Q8GUK6, Q8LBA6, Q8SX37, Q8VDP6, Q8XFD0, A1JLU9, A4TK40, P45419, Q1C8L0, Q1CHE5, Q2NTS8, Q492P7, Q66BN4, Q6D364, Q7VR12, Q8H8U0, Q8ZF51, A0A2K3D1C8

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	4
Likely pathogenic	1
Uncertain significance	22
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (5)

Variant ID	HGVS	Classification
2576522	GRCh37/hg19 16p11.2(chr16:29656684-30197341)x1	Pathogenic
625610	GRCh37/hg19 16p11.2(chr16:29827174-30198041)	Pathogenic
979440	GRCh37/hg19 16p11.2(chr16:28488319-30178406)x1	Pathogenic
997050	GRCh37/hg19 16p11.2(chr16:29652999-30197341)	Pathogenic
223114	NC_000016.10:g.(?29602174)(30178709_?)dup	Likely pathogenic

SpliceAI

526 predictions. Top by Δscore:

Variant	Effect	Δscore
16:29859335:C:CC	acceptor_gain	1.0000
16:29859436:TCCTA:T	donor_loss	1.0000
16:29859437:CCTA:C	donor_loss	1.0000
16:29859438:CTA:C	donor_loss	1.0000
16:29859439:TA:T	donor_loss	1.0000
16:29859440:A:C	donor_loss	1.0000
16:29859441:CCT:C	donor_loss	1.0000
16:29859519:GCAGG:G	acceptor_gain	1.0000
16:29859520:CAGG:C	acceptor_gain	1.0000
16:29859520:CAGGC:C	acceptor_gain	1.0000
16:29859521:AGG:A	acceptor_gain	1.0000
16:29859522:GG:G	acceptor_gain	1.0000
16:29859523:GC:G	acceptor_loss	1.0000
16:29859524:C:CC	acceptor_gain	1.0000
16:29859525:T:A	acceptor_loss	1.0000
16:29860575:GCTTA:G	donor_loss	1.0000
16:29860576:CTTA:C	donor_loss	1.0000
16:29860577:TTA:T	donor_loss	1.0000
16:29860578:TAC:T	donor_loss	1.0000
16:29860579:A:AC	donor_gain	1.0000
16:29860579:A:T	donor_loss	1.0000
16:29860579:AC:A	donor_gain	1.0000
16:29860579:ACC:A	donor_gain	1.0000
16:29860579:ACCCT:A	donor_gain	1.0000
16:29860580:C:CC	donor_gain	1.0000
16:29860580:CC:C	donor_gain	1.0000
16:29860580:CCC:C	donor_gain	1.0000
16:29860580:CCCT:C	donor_gain	1.0000
16:29860580:CCCTC:C	donor_gain	1.0000
16:29860658:CAGAA:C	acceptor_gain	1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000556536 (16:29863854 A>G), RS1000672613 (16:29860240 C>T), RS1001874080 (16:29858013 C>T), RS1002426899 (16:29864478 C>T), RS1003247056 (16:29862917 C>G), RS1004371785 (16:29860340 C>A), RS1004669238 (16:29863001 G>A), RS1004697166 (16:29863210 A>T), RS1005781941 (16:29861768 C>G), RS1006336815 (16:29864176 G>A,C), RS1006367852 (16:29864410 C>A), RS1006376896 (16:29863314 G>T), RS1006714191 (16:29859970 A>T), RS1006864939 (16:29861874 C>T), RS1007289436 (16:29862172 C>T)

Disease associations

OMIM: gene MIM:605893 | disease phenotypes: MIM:611913, MIM:614671

GenCC curated gene-disease

Mondo (3): autism spectrum disorder (MONDO:0005258), proximal 16p11.2 microdeletion syndrome (MONDO:0012756), chromosome 16p11.2 duplication syndrome (MONDO:0013847)

Orphanet (3): Proximal 16p11.2 microdeletion syndrome (Orphanet:261197), Proximal 16p11.2 microduplication syndrome (Orphanet:370079), NON RARE IN EUROPE: Autism (Orphanet:106)

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST004599_109	Mean platelet volume	2.000000e-09

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
C579850	16p11.2 Deletion Syndrome (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6067053 (SINGLE PROTEIN)

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

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
9.00	Kd	0.993	nM	CHEMBL3752910
9.00	ED50	0.993	nM	CHEMBL3752910
7.24	Kd	58.09	nM	CHEMBL5653589
7.24	ED50	58.09	nM	CHEMBL5653589

PubChem BioAssay actives

2 with measured affinity, of 4 total; 2 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148041: Binding affinity to human CDIPT incubated for 45 mins by Kinobead based pull down assay	kd	0.0010	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148041: Binding affinity to human CDIPT incubated for 45 mins by Kinobead based pull down assay	kd	0.0581	uM

CTD chemical–gene interactions

25 total (human), top 25 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	increases expression, affects cotreatment	3
Air Pollutants	affects expression, increases abundance, decreases expression	2
Valproic Acid	increases expression, increases methylation	2
Cyclosporine	decreases expression	2
Particulate Matter	decreases expression, increases abundance, increases expression	2
triphenyl phosphate	affects expression	1
beta-lapachone	increases expression	1
sodium arsenite	affects binding, increases reaction	1
CGP 52608	affects binding, increases reaction	1
bisphenol B	increases expression	1
MT19c compound	decreases expression	1
3-(2-hydroxy-4-(2-methylnonan-2-yl)phenyl)cyclohexan-1-ol	increases expression	1
bisphenol AF	increases expression	1
Vehicle Emissions	increases abundance, increases expression	1
Clozapine	increases expression	1
Dexamethasone	affects cotreatment, increases expression	1
Fluorouracil	affects expression	1
Indomethacin	affects cotreatment, increases expression	1
Ivermectin	decreases expression	1
Ozone	affects expression, increases abundance	1
Rotenone	decreases expression	1
Smoke	decreases expression	1
Tobacco Smoke Pollution	increases expression	1
Urethane	increases expression	1
1-Methyl-3-isobutylxanthine	increases expression, affects cotreatment	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5651083	Binding	Binding affinity to human CDIPT incubated for 45 mins by Kinobead based pull down assay	NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00391261	PHASE4	COMPLETED	An Open-label Trial of Metformin for Weight Control of Pediatric Patients on Antipsychotic Medications.
NCT01028820	PHASE4	COMPLETED	FMRI Brain Activation of Aripiprazole Treatment in Autism Spectrum Disorders
NCT01333865	PHASE4	COMPLETED	A Study of Memantine Hydrochloride (Namenda®) for Cognitive and Behavioral Impairment in Adults With Autism Spectrum Disorders
NCT01337700	PHASE4	COMPLETED	Milnacipran in Autism and the Functional Locus Coeruleus and Noradrenergic Model of Autism
NCT01695200	PHASE4	COMPLETED	Omega-3 Fatty Acids in Autism Spectrum Disorders
NCT02096952	PHASE4	COMPLETED	Methylphenidate ER Liquid Formulation in Adults With ASD and ADHD
NCT02235467	PHASE4	COMPLETED	Multisite Study: Parental Training Using Video Modelling to Develop Social Skills in Children With Autism
NCT02940574	PHASE4	COMPLETED	Neural and Behavioral Effects of Oxytocin in Autism Spectrum Disorders
NCT03333629	PHASE4	COMPLETED	Promoting Positive Outcomes for Individuals With ASD: Linking Early Detection, Treatment, and Long-term Outcomes
NCT03337646	PHASE4	COMPLETED	Evaluation of the Effect and Safety of Lisdexamfetamine in Children Aged 6-12 With ADHD and Autism
NCT03538431	PHASE4	COMPLETED	Improving Driving in Young People With Autism Spectrum Disorders
NCT03757585	PHASE4	COMPLETED	Natural Treatments for the Management of Emotional Dysregulation in Youth With Non-verbal Learning Disability (NVLD) and/or Autism Spectrum Disorders (ASD)
NCT04903353	PHASE4	COMPLETED	Pragmatic Trial Comparing Weight Gain in Children With Autism Taking Risperidone Versus Aripiprazole
NCT05063656	PHASE4	COMPLETED	Biomarker-Driven Pharmacological Treatment of Adolescents With Autism Spectrum Disorder With Gabapentin
NCT05146245	PHASE4	UNKNOWN	Safety and Pharmacokinetics of Antipsychotics in Children 2: Studying TDM in an RCT
NCT05916339	PHASE4	RECRUITING	AWARE: Management of ADHD in Autism Spectrum Disorder
NCT05954052	PHASE4	TERMINATED	A Study of Glutathione in Children With Autism Spectrum Disorder
NCT06853665	PHASE4	RECRUITING	The TEAM Study - Treatment Efficacy for Autism/Attention Using Mixed Amphetamine
NCT07054697	PHASE4	COMPLETED	Pilot-RCT With Individualized Homeopathic Treatment in the Children With Autism Spectrum Disorder
NCT07161804	PHASE4	COMPLETED	Pilot RCT Using Homeopathic Medicines in ASD
NCT07439042	PHASE4	NOT_YET_RECRUITING	Buspirone for Anxiety in Autistic Youth
NCT01302964	PHASE3	COMPLETED	Mirtazapine Treatment of Anxiety in Children and Adolescents With Pervasive Developmental Disorders
NCT01706523	PHASE3	TERMINATED	Open Label Extension Study of STX209 (Arbaclofen) in Autism Spectrum Disorders
NCT01825798	PHASE3	COMPLETED	Treatment of Overweight Induced by Antipsychotic Medication in Young People With Autism Spectrum Disorders (ASD)
NCT01972074	PHASE3	COMPLETED	Behavioral and Neural Response to Memantine in Adolescents With Autism Spectrum Disorder
NCT02985749	PHASE3	COMPLETED	A Study of Oxytocin for the Treatment of Social Impairment in Individuals With High Functioning Autism Spectrum Disorder
NCT03197922	PHASE3	COMPLETED	Treatment of Encopresis in Children With Autism Spectrum Disorders
NCT03504917	PHASE3	TERMINATED	A Study of Balovaptan in Adults With Autism Spectrum Disorder With a 2-Year Open-Label Extension
NCT03553875	PHASE3	TERMINATED	Memantine for the Treatment of Social Deficits in Youth With Disorders of Impaired Social Interactions
NCT03640156	PHASE3	COMPLETED	Modulating Socially Adaptive Mirror System Functioning in Autism by Oxytocin
NCT03715153	PHASE3	TERMINATED	Efficacy and Safety of Bumetanide Oral Liquid Formulation in Children Aged From 2 to Less Than 7 Years Old With Autism Spectrum Disorder.
NCT03715166	PHASE3	TERMINATED	Efficacy and Safety of Bumetanide Oral Liquid Formulation in Children and Adolescents Aged From 7 to Less Than 18 Years Old With Autism Spectrum Disorder
NCT04233502	PHASE3	WITHDRAWN	Efficacy and Safety of Slenyto for Insomnia in Children With ASD
NCT04578756	PHASE3	COMPLETED	Open-Label, Flexible-dose Study to Evaluate the Long-Term Safety and Tolerability of Cariprazine in the Treatment of Pediatric Participants With Schizophrenia, Bipolar I Disorder, or Autism Spectrum Disorder
NCT04623398	PHASE3	COMPLETED	Effect of Lithium in Patients With Autism Spectrum Disorder and Phelan-McDermid Syndrome (SHANK3 Haploinsufficiency)
NCT04725383	PHASE3	TERMINATED	Amitriptyline for Repetitive Behaviors in Autism Spectrum Disorders
NCT05212493	PHASE3	COMPLETED	The Effects of Medical Cannabis in Children With Autistic Spectrum Disorder
NCT05361707	PHASE3	UNKNOWN	Evaluating the Effects of Tasimelteon in Individuals With Autism Spectrum Disorder (ASD) and Sleep Disturbances
NCT05439616	PHASE3	COMPLETED	Study of Cariprazine Oral Capsules or Solution to Assess Adverse Events and Change in Irritability Due to Autism Spectrum Disorder (ASD) in Participants Aged 5-17 Years With ASD
NCT06229210	PHASE3	RECRUITING	Safety and Tolerability Trial of Lumateperone in Pediatric Patients With Schizophrenia, Bipolar Disorder or Autism Spectrum Disorder