CEP-1347

Summary

Cep-1347 (CHEMBL290352) is a phase-3 clinical-stage small molecule targeting MAP3K10, MAP3K11, and MAP3K12; indicated across 1 condition including parkinson disease.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 4 (MAP3K10, MAP3K11, MAP3K12…)
• Indications: 1 condition
• Clinical trials: 1
• Chemistry: 615.8 Da · C33H33N3O5S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL290352
Name	CEP-1347
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9917013
Molecular formula	C33H33N3O5S2
Molecular weight	615.8
InChIKey	SCMLRESZJCKCTC-KMYQRJGFSA-N

SMILES: CCSCC1=CC2=C(C=C1)N3[C@H]4C[C@@]([C@](O4)(N5C6=C(C=C(C=C6)CSCC)C7=C8CNC(=O)C8=C2C3=C75)C)(C(=O)OC)O

IUPAC name: methyl (15S,16R,18R)-10,23-bis(ethylsulfanylmethyl)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8(13),9,11,20(25),21,23,26-nonaene-16-carboxylate

Also known as: Cep-1347, KT-1575, KT-7515, KT7515, Indolocarbazole analogue, CEP-1347, NA

Patent coverage: 153 distinct patent families (359 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 338 (94%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
MAP3K10	mitogen-activated protein kinase kinase kinase 10	Inhibition	8.7	0.2%	Q02779
MAP3K11	mitogen-activated protein kinase kinase kinase 11	Inhibition	8.22	8.7%	Q16584
MAP3K12	mitogen-activated protein kinase kinase kinase 12	Inhibition	6.94	0.3%	Q12852
MAP3K9	mitogen-activated protein kinase kinase kinase 9	Inhibition	9	0.1%	P80192

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Vascular endothelial growth factor receptor 1, Vascular endothelial growth factor receptor 3, Mitogen-activated protein kinase kinase kinase 11, Vascular endothelial growth factor receptor 2, Mitogen-activated protein kinase kinase kinase 9, Mitogen-activated protein kinase kinase kinase 10, Protein delta homolog 1.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
MAP3K10	8.7	IC50	2	nM	CHEMBL_ACT_13476493
MAP3K11	8.22	IC50	6	nM	CHEMBL_ACT_13476474
MAP3K11	7.64	IC50	23	nM	CHEMBL_ACT_18550755
MAP3K11	7.64	IC50	23.1	nM	CHEMBL_ACT_215499
MAP3K11	7.64	IC50	23	nM	CHEMBL_ACT_25521010
MAP3K9	7.42	IC50	38	nM	CHEMBL_ACT_18550759
MAP3K9	7.42	IC50	38	nM	CHEMBL_ACT_215497
MAP3K9	7.42	IC50	38	nM	CHEMBL_ACT_2379701
MAP3K9	7.42	IC50	38	nM	CHEMBL_ACT_25516697
FLT4	7.41	IC50	39	nM	CHEMBL_ACT_2379813
KDR	7.37	IC50	43	nM	CHEMBL_ACT_2379812
MAP3K10	7.29	IC50	51	nM	CHEMBL_ACT_18550757
MAP3K10	7.29	IC50	51	nM	CHEMBL_ACT_215498
MAP3K10	7.29	IC50	51	nM	CHEMBL_ACT_25516698
MAP3K11	7.19	IC50	64	nM	CHEMBL_ACT_2379720
MAP3K9	7.14	IC50	72	nM	CHEMBL_ACT_2379739
DLK1	6.94	IC50	114	nM	CHEMBL_ACT_18550760
DLK1	6.94	IC50	114	nM	CHEMBL_ACT_2379753
FLT1	6.68	IC50	209	nM	CHEMBL_ACT_2379700

Target pathways

Aggregated over 4 target gene(s): MAP3K10, MAP3K11, MAP3K12, MAP3K9.

Top Reactome pathways

18 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	MAP3K11
Disease	1	MAP3K11
Signaling by Rho GTPases	1	MAP3K11
Diseases of signal transduction by growth factor receptors and second messengers	1	MAP3K11
RAF activation	1	MAP3K11
RAF/MAP kinase cascade	1	MAP3K11
MAPK family signaling cascades	1	MAP3K11
MAPK1/MAPK3 signaling	1	MAP3K11
Signaling by moderate kinase activity BRAF mutants	1	MAP3K11
Signaling by RAS mutants	1	MAP3K11
Paradoxical activation of RAF signaling by kinase inactive BRAF	1	MAP3K11
Oncogenic MAPK signaling	1	MAP3K11
RHO GTPase cycle	1	MAP3K11
CDC42 GTPase cycle	1	MAP3K11
RHOG GTPase cycle	1	MAP3K11
RHOV GTPase cycle	1	MAP3K11
Signaling downstream of RAS mutants	1	MAP3K11
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	1	MAP3K11

Dominant GO biological processes

GO term	Targets
protein autophosphorylation	4
protein phosphorylation	4
JNK cascade	3
positive regulation of apoptotic process	3
apoptotic process	2
signal transduction	2
positive regulation of JUN kinase activity	2
positive regulation of JNK cascade	2
MAPK cascade	2
smoothened signaling pathway	1
peptidyl-serine phosphorylation	1
peptidyl-threonine phosphorylation	1
obsolete negative regulation of DNA-binding transcription factor activity	1
negative regulation of DNA-templated transcription	1
microtubule-based process	1

Indications & clinical

Indications

1 indication (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
Parkinson disease	2	MONDO:0005180	MONDO:0005180

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00040404	PHASE2/PHASE3	TERMINATED	Safety and Efficacy Study of CEP-1347 in the Treatment of Parkinson’s Disease

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

86 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Axitinib	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Bosutinib	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Crizotinib	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
FEDRATINIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
MIDOSTAURIN	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
NERATINIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Ruxolitinib	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Sunitinib	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
NINTEDANIB	ChEMBL	Phase 4 (approved)	MAP3K10, MAP3K11, MAP3K12, MAP3K9
DOVITINIB	ChEMBL	Phase 3	MAP3K10, MAP3K11, MAP3K12, MAP3K9
LESTAURTINIB	ChEMBL	Phase 3	MAP3K10, MAP3K11, MAP3K12, MAP3K9
FORETINIB	ChEMBL	Phase 2	MAP3K10, MAP3K11, MAP3K12, MAP3K9
TOZASERTIB	ChEMBL	Phase 2	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Abemaciclib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Acalabrutinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Afatinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Duvelisib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Erlotinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Gefitinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Idelalisib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Imatinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Lapatinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Nilotinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Quizartinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Selumetinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Sorafenib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
Vandetanib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12, MAP3K9
R-406	ChEMBL	Phase 2	MAP3K10, MAP3K11, MAP3K9
SU-014813	ChEMBL	Phase 2	MAP3K11, MAP3K12, MAP3K9
Tofacitinib	PubChem	Approved	MAP3K10, MAP3K11, MAP3K12
ALVOCIDIB	ChEMBL	Phase 3	MAP3K10, MAP3K9
DEFACTINIB	ChEMBL	Phase 3	MAP3K11, MAP3K9
REBASTINIB	ChEMBL	Phase 2	MAP3K11, MAP3K9
Cobimetinib	PubChem	Approved	MAP3K11, MAP3K9
Momelotinib	PubChem	Approved	MAP3K11, MAP3K9
Osimertinib	PubChem	Approved	MAP3K11, MAP3K9
Sirolimus	PubChem	Approved	MAP3K11, MAP3K9
BRIGATINIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K9
CAPIVASERTIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K11
DABRAFENIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K11
DASATINIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K10
ENCORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K11
FOSTAMATINIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K11
GILTERITINIB	ChEMBL + PubChem	Phase 4 (approved)	MAP3K11
CRENOLANIB	ChEMBL	Phase 3	MAP3K11
ORANTINIB	ChEMBL	Phase 3	MAP3K11
RUBOXISTAURIN	ChEMBL	Phase 3	MAP3K9
ADAVOSERTIB	ChEMBL	Phase 2	MAP3K11
APITOLISIB	ChEMBL	Phase 2	MAP3K9
AT-9283	ChEMBL	Phase 2	MAP3K11
BERZOSERTIB	ChEMBL	Phase 2	MAP3K9
BMS-690514	ChEMBL	Phase 2	MAP3K11
CERDULATINIB	ChEMBL	Phase 2	MAP3K9
MILCICLIB	ChEMBL	Phase 2	MAP3K11
RAF-265	ChEMBL	Phase 2	MAP3K11
SILMITASERTIB	ChEMBL	Phase 2	MAP3K11
UCN-01	ChEMBL	Phase 2	MAP3K11
Alectinib	PubChem	Approved	MAP3K11
Alpelisib	PubChem	Approved	MAP3K11