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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Ligand
BDBM8037
Substrate
GST-Rb fusion protein
Meas. Tech.
CDK Kinase Inhibition Assay
Temperature
303.1500±n/a K
Ki
16000±n/a nM
Comments
extracted
Citation
 Wang, S; Meades, C; Wood, G; Osnowski, A; Anderson, S; Yuill, R; Thomas, M; Mezna, M; Jackson, W; Midgley, C; Griffiths, G; Fleming, I; Green, S; McNae, I; Wu, SY; McInnes, C; Zheleva, D; Walkinshaw, MD; Fischer, PM 2-Anilino-4-(thiazol-5-yl)pyrimidine CDK inhibitors: synthesis, SAR analysis, X-ray crystallography, and biological activity. J Med Chem 47:1662-75 (2004) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Synonyms:
CDK4/CycD | CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | Cyclin-dependent kinase 4 | Cyclin-Dependent Kinase 4 (CDK4) | Cyclin-dependent kinase 4/cyclin D1 | Cyclin-dependent kinase 4/G1/S-specific cyclin D1
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
CDK4/D1 complexes were purified from insect cells co-infected with baculovirus vectors containing each of the components.
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-dependent kinase 4
Synonyms:
Cell division protein kinase 4 | Cyclin-dependent kinase 4 (CDK 4) | PSK-J3 | CDK4_HUMAN | CDK4
Type:
Enzyme Subunit
Mol. Mass.:
33731.96
Organism:
Human
Description:
P11802
Residue:
303
Sequence:
MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALLRRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDLMRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWYRAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPRDVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEGNPE
  
Component 2
Name:
G1/S-specific cyclin-D1
Synonyms:
B-cell lymphoma 1 protein | BCL-1 oncogene | BCL-1 | PRAD1 oncogene | CCND1_HUMAN | CCND1 | BCL1 | PRAD1
Type:
Enzyme Subunit
Mol. Mass.:
33717.70
Organism:
Human
Description:
n/a
Residue:
295
Sequence:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIVATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLTAEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRKHAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCDPDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
  
Inhibitor
Name:
BDBM8037
Synonyms:
4-(2,4-dimethyl-1,3-thiazol-5-yl)pyrimidin-2-amine | 4-(dimethyl-1,3-thiazol-5-yl)pyrimidin-2-amine, 1 | CS12 | 4-(2,4-Dimethylthiazol-5-yl)pyrimidin-2-ylamine | 2-Anilino-4-(thiazol-5-yl)pyrimidine deriv. 8
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
GST-Rb fusion protein
Synonyms:
RB_HUMAN | RB1 | Glutathione S-transferase (GST)-retinoblastoma (Rb) fusion | Histidine-tagged retinoblastoma protein | Rb | retinoblastoma
Type:
Other Protein Type
Mol. Mass.:
106410.17
Organism:
Human
Description:
GST-60 kDa Rb fusion protein (comprising amino acids 378 to 928 of retinoblastoma)
Residue:
928
Sequence:
MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTALCQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIARVDLDEMSFTLLSYRKTYEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSSISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYKTAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFMNSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDRRLFLDHDKTLQTDSIDSFETQRTPRKSNLDEEVNIIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVKDIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDNIFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEGNLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNHTAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYLRLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLKFKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMDTSNKEEK