Reaction Details |
| Report a problem with these data |
Target | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 |
---|
Ligand | BDBM12618 |
---|
Substrate/Competitor | GST-Rb fusion protein |
---|
Meas. Tech. | Homogeneous Time-resolved Fluorescence (HTRF) Assay |
---|
Ki | 36±n/a nM |
---|
Citation | Chu, XJ; DePinto, W; Bartkovitz, D; So, SS; Vu, BT; Packman, K; Lukacs, C; Ding, Q; Jiang, N; Wang, K; Goelzer, P; Yin, X; Smith, MA; Higgins, BX; Chen, Y; Xiang, Q; Moliterni, J; Kaplan, G; Graves, B; Lovey, A; Fotouhi, N Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity. J Med Chem49:6549-60 (2006) [PubMed] Article |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 |
---|
Name: | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 |
Synonyms: | CDK4/CycD | CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | Cyclin-Dependent Kinase 4 (CDK4) | Cyclin-dependent kinase 4 | Cyclin-dependent kinase 4/G1/S-specific cyclin D1 | Cyclin-dependent kinase 4/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: | CDK4 | CDK4_HUMAN | Cell division protein kinase 4 | Cyclin-dependent kinase 4 (CDK 4) | PSK-J3 |
Type: | Enzyme Subunit |
Mol. Mass.: | 33731.96 |
Organism: | Homo sapiens (Human) |
Description: | P11802 |
Residue: | 303 |
Sequence: | MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALL
RRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDL
MRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWY
RAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPR
DVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEG
NPE
|
|
|
Component 2 |
Name: | G1/S-specific cyclin-D1 |
Synonyms: | B-cell lymphoma 1 protein | BCL-1 | BCL-1 oncogene | BCL1 | CCND1 | CCND1_HUMAN | PRAD1 | PRAD1 oncogene |
Type: | Enzyme Subunit |
Mol. Mass.: | 33717.70 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 295 |
Sequence: | MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIV
ATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLT
AEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRK
HAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCD
PDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
|
|
|
BDBM12618 |
---|
GST-Rb fusion protein |
---|
Name: | GST-Rb fusion protein |
Synonyms: | Glutathione S-transferase (GST)-retinoblastoma (Rb) fusion | Histidine-tagged retinoblastoma protein | RB1 | RB_HUMAN | Rb | retinoblastoma |
Type: | Other Protein Type |
Mol. Mass.: | 106410.17 |
Organism: | Homo sapiens (Human) |
Description: | GST-60 kDa Rb fusion protein (comprising amino acids 378 to 928 of retinoblastoma) |
Residue: | 928 |
Sequence: | MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTAL
CQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIARVDLDEMSFTLLSY
RKTYEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSS
ISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYK
TAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFM
NSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDRRLFLDHDKTLQTDSIDSFETQRTPRKS
NLDEEVNIIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVK
DIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDN
IFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEG
NLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNH
TAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYL
RLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLK
FKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLS
PIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFG
TSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQK
LAEMTSTRTRMQKQKMNDSMDTSNKEEK
|
|
|