cell division cycle 7 | CDC7 family | IUPHAR/BPS Guide to PHARMACOLOGY

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cell division cycle 7

Target not currently curated in GtoImmuPdb

Target id: 1960

Nomenclature: cell division cycle 7

Abbreviated Name: CDC7

Family: CDC7 family

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 574 1p22 CDC7 cell division cycle 7
Mouse - 564 5 E Cdc7 cell division cycle 7 (S. cerevisiae)
Rat - 565 14p22 Cdc7 cell division cycle 7
Previous and Unofficial Names
CDC7-related kinase | Hsk1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Human CDC7 kinase in complex with DBF4 and XL413
PDB Id:  4F9C
Resolution:  2.08Å
Species:  Human
References:  2
Enzyme Reaction
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 89S [PMID: 19115845] Hs Inhibition 9.3 pKi 5
pKi 9.3 (Ki 5x10-10 M) [5]
compound 2 [PMID: 22560567] Hs Inhibition 8.9 pIC50 3
pIC50 8.9 (IC50 1.4x10-9 M) [3]
compound 89S [PMID: 19115845] Hs Inhibition 8.7 pIC50 5
pIC50 8.7 (IC50 2x10-9 M) [5]
XL413 Hs Inhibition 8.5 pIC50 3
pIC50 8.5 (IC50 3.4x10-9 M) [3]
compound 74 [PMID: 24793884] Hs Inhibition 8.4 pIC50 6
pIC50 8.4 (IC50 3.77x10-9 M) [6]
compound 77 [PMID: 24793884] Hs Inhibition 8.2 pIC50 6
pIC50 8.2 (IC50 6.81x10-9 M) [6]
compound 18 [PMID: 20873740] Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 2.2x10-8 M) [4]
compound 1 [PMID: 24793884] Hs Inhibition 6.5 pIC50 6
pIC50 6.5 (IC50 3.23x10-7 M) [6]
TAK-931 Hs Inhibition - - 1
Inhibits CDC7/Dbf4 complex activity by 103 % in a proprietary HTRF ADP formation assay (Transcreener, Cisbio) [1]

References

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1. Homma M, Miyazaki T, Oguru Y, Kurasawa O. (2017) Heterocyclic compound. Patent number: US9655900B2. Assignee: Takeda Pharmaceutical Co Ltd. Priority date: 17/02/2010. Publication date: 23/05/2017.

2. Hughes S, Elustondo F, Di Fonzo A, Leroux FG, Wong AC, Snijders AP, Matthews SJ, Cherepanov P. (2012) Crystal structure of human CDC7 kinase in complex with its activator DBF4. Nat. Struct. Mol. Biol., 19 (11): 1101-7. [PMID:23064647]

3. Koltun ES, Tsuhako AL, Brown DS, Aay N, Arcalas A, Chan V, Du H, Engst S, Ferguson K, Franzini M et al.. (2012) Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg. Med. Chem. Lett., 22 (11): 3727-31. [PMID:22560567]

4. Menichincheri M, Albanese C, Alli C, Ballinari D, Bargiotti A, Caldarelli M, Ciavolella A, Cirla A, Colombo M, Colotta F et al.. (2010) Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding. J. Med. Chem., 53 (20): 7296-315. [PMID:20873740]

5. Menichincheri M, Bargiotti A, Berthelsen J, Bertrand JA, Bossi R, Ciavolella A, Cirla A, Cristiani C, Croci V, D'Alessio R et al.. (2009) First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J. Med. Chem., 52 (2): 293-307. [PMID:19115845]

6. Reichelt A, Bailis JM, Bartberger MD, Yao G, Shu H, Kaller MR, Allen JG, Weidner MF, Keegan KS, Dao JH. (2014) Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. Eur J Med Chem, 80: 364-82. [PMID:24793884]

How to cite this page

CDC7 family: cell division cycle 7. Last modified on 08/03/2019. Accessed on 26/02/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1960.