Target Information

Target General Infomation
Target ID
T81358
Former ID
TTDI02039
Target Name
CDC7 protein kinase
Gene Name
CDC7
Synonyms
CDC7related kinase; Cell division cycle 7related protein kinase; HsCdc7; huCdc7; CDC7
Target Type
Clinical Trial
Disease Hematological malignancies [ICD9: 200-209; ICD10: C81-C86]
Function
Seems to phosphorylate critical substrates that regulate the G1/S phase transition and/or DNA replication. Can phosphorylates MCM2 and MCM3.
BioChemical Class
Kinase
UniProt ID
O00311
EC Number
EC 2.7.11.1
Sequence
MEASLGIQMDEPMAFSPQRDRFQAEGSLKKNEQNFKLAGVKKDIEKLYEAVPQLSNVFKI
EDKIGEGTFSSVYLATAQLQVGPEEKIALKHLIPTSHPIRIAAELQCLTVAGGQDNVMGV
KYCFRKNDHVVIAMPYLEHESFLDILNSLSFQEVREYMLNLFKALKRIHQFGIVHRDVKP
SNFLYNRRLKKYALVDFGLAQGTHDTKIELLKFVQSEAQQERCSQNKSHIITGNKIPLSG
PVPKELDQQSTTKASVKRPYTNAQIQIKQGKDGKEGSVGLSVQRSVFGERNFNIHSSISH
ESPAVKLMKQSKTVDVLSRKLATKKKAISTKVMNSAVMRKTASSCPASLTCDCYATDKVC
SICLSRRQQVAPRAGTPGFRAPEVLTKCPNQTTAIDMWSAGVIFLSLLSGRYPFYKASDD
LTALAQIMTIRGSRETIQAAKTFGKSILCSKEVPAQDLRKLCERLRGMDSSTPKLTSDIQ
GHASHQPAISEKTDHKASCLVQTPPGQYSGNSFKKGDSNSCEHCFDEYNTNLEGWNEVPD
EAYDLLDKLLDLNPASRITAEEALLHPFFKDMSL
Drugs and Mode of Action
Drug(s) BMS-863233 Drug Info Phase 1/2 Hematological malignancies [522575], [542978]
Modulator BMS-863233 Drug Info [531895]
PHA-767491 Drug Info
Inhibitor compound 1 Drug Info [532762]
compound 18 Drug Info [531180]
compound 2 Drug Info [531895]
compound 74 Drug Info [532762]
compound 77 Drug Info [532762]
compound 89S Drug Info [529892]
Pathways
NetPath Pathway TGF_beta_Receptor Signaling Pathway
References
Ref 522575ClinicalTrials.gov (NCT00838890) A Study of BMS-863233 in Patients With Hematologic Cancer. U.S. National Institutes of Health.
Ref 542978(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8113).
Ref 529892First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem. 2009 Jan 22;52(2):293-307.
Ref 531180Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. J Med Chem. 2010 Oct 28;53(20):7296-315.
Ref 531895Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31.
Ref 532762Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. Eur J Med Chem. 2014 Jun 10;80:364-82.

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