Reaction Details Report a problem with these data
Target
Cyclin-dependent kinase 2
Ligand
BDBM370121
Substrate
n/a
Meas. Tech.
ChEMBL_2276759
EC50
9.0±n/a nM
Citation
Freeman-Cook, KD; Hoffman, RL; Behenna, DC; Boras, B; Carelli, J; Diehl, W; Ferre, RA; He, YA; Hui, A; Huang, B; Huser, N; Jones, R; Kephart, SE; Lapek, J; McTigue, M; Miller, N; Murray, BW; Nagata, A; Nguyen, L; Niessen, S; Ninkovic, S; O'Doherty, I; Ornelas, MA; Solowiej, J; Sutton, SC; Tran, K; Tseng, E; Visswanathan, R; Xu, M; Zehnder, L; Zhang, Q; Zhang, C; Dann, S Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer. J Med Chem 64:9056-9077 (2021) [PubMed]
More Info.:
Target
Name:
Cyclin-dependent kinase 2
Synonyms:
CDK2 | CDK2-Kinase | CDK2_HUMAN | CDKN2 | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | Protein cereblon/Cyclin-dependent kinase 2 | p33 protein kinase
Type:
Enzyme Subunit
Mol. Mass.:
33938.17
Organism:
Homo sapiens (Human)
Description:
P24941
Residue:
298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
Inhibitor
Name:
BDBM370121
Synonyms:
6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one | US10233188, Example 10 | US10800783, Example 10 | US11396512, Example 10
Type:
Small organic molecule
Emp. Form.:
C20H27F2N5O4S
Mol. Mass.:
471.521
SMILES:
C[C@@]1(O)CCC[C@H]1n1c2nc(NC3CCN(CC3)S(C)(=O)=O)ncc2cc(C(F)F)c1=O |r|