Top ▲

cell division cycle 7

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 1960

Nomenclature: cell division cycle 7

Abbreviated Name: CDC7

Family: CDC7 family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 574 1p22.1 CDC7 cell division cycle 7
Mouse - 564 5 E5 Cdc7 cell division cycle 7
Rat - 565 14p22 Cdc7 cell division cycle 7
Previous and Unofficial Names Click here for help
CDC7-related kinase | Hsk1
Database Links Click here for help
Alphafold O00311 (Hs), Q9Z0H0 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5443 (Hs)
Ensembl Gene ENSG00000097046 (Hs), ENSMUSG00000029283 (Mm), ENSRNOG00000002105 (Rn)
Entrez Gene 8317 (Hs), 12545 (Mm), 360908 (Rn)
Human Protein Atlas ENSG00000097046 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:8317 (Hs), mmu:12545 (Mm), rno:360908 (Rn)
OMIM 603311 (Hs)
Pharos O00311 (Hs)
RefSeq Nucleotide NM_001134419 (Hs), NM_001271566 (Mm), NM_001108352 (Rn)
RefSeq Protein NP_001127891 (Hs), NP_001258495 (Mm), NP_001101822 (Rn)
SynPHARM 81366 (in complex with XL413)
UniProtKB O00311 (Hs), Q9Z0H0 (Mm)
Wikipedia CDC7 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file go icon to follow link

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] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.3 pKi 6
⤷ pKi 9.3 (Ki 5x10-10 M) [6]
compound 2 [PMID: 22560567] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.9 pIC50 4
⤷ pIC50 8.9 (IC50 1.4x10-9 M) [4]
compound 89S [PMID: 19115845] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 6
⤷ pIC50 8.7 (IC50 2x10-9 M) [6]
monzosertib Small molecule or natural product Hs Inhibition 8.6 pIC50 3
⤷ pIC50 8.6 (IC50 2.4x10-9 M) [3]
XL413 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 4
⤷ pIC50 8.5 (IC50 3.4x10-9 M) [4]
compound 74 [PMID: 24793884] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 7
⤷ pIC50 8.4 (IC50 3.77x10-9 M) [7]
compound 77 [PMID: 24793884] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 7
⤷ pIC50 8.2 (IC50 6.81x10-9 M) [7]
compound 18 [PMID: 20873740] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.7 pIC50 5
⤷ pIC50 7.7 (IC50 2.2x10-8 M) [5]
compound 1 [PMID: 24793884] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.5 pIC50 7
⤷ pIC50 6.5 (IC50 3.23x10-7 M) [7]
simurosertib Small molecule or natural product Ligand has a PDB structure Hs Inhibition - - 1
⤷ Inhibits CDC7/Dbf4 complex activity by 103 % in a proprietary HTRF ADP formation assay (Transcreener, Cisbio) [1]

References

Show »

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. Irie T, Asami T, Sawa A, Uno Y, Taniyama C, Funakoshi Y, Masai H, Sawa M. (2021) Discovery of AS-0141, a Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers. J Med Chem, 64 (19): 14153-14164. [PMID:34607435]

4. 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]

5. 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]

6. 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]

7. 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 06/10/2021. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1960.