Reaction Details |
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Target | CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7 |
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Ligand | BDBM5655 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1614445 (CHEMBL3856514) |
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IC50 | 514±n/a nM |
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Citation | Sonawane, YA; Taylor, MA; Napoleon, JV; Rana, S; Contreras, JI; Natarajan, A Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. J Med Chem59:8667-8684 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7 |
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Name: | CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7 |
Synonyms: | CDK-activating kinase assembly factor MAT1/Cyclin H/Cyclin-dependent kinase 7 | CDK7/Cyclin H/MNAT1 |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 3 components. |
Component 1 |
Name: | Cyclin-dependent kinase 7 |
Synonyms: | 39 kDa protein kinase | CAK | CAK1 | CDK-activating kinase | CDK-activating kinase 1 (CAK) | CDK7 | CDK7_HUMAN | CDKN7 | Cell division protein kinase 7 | Cyclin-Dependent Kinase 7 (CDK7) | Cyclin-dependent kinase 7 (CDK7/cyclin H) | MO15 | P39 Mo15 | STK1 | TFIIH basal transcription factor complex kinase subunit |
Type: | Enzyme Subunit |
Mol. Mass.: | 39047.01 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 346 |
Sequence: | MALDVKSRAKRYEKLDFLGEGQFATVYKARDKNTNQIVAIKKIKLGHRSEAKDGINRTAL
REIKLLQELSHPNIIGLLDAFGHKSNISLVFDFMETDLEVIIKDNSLVLTPSHIKAYMLM
TLQGLEYLHQHWILHRDLKPNNLLLDENGVLKLADFGLAKSFGSPNRAYTHQVVTRWYRA
PELLFGARMYGVGVDMWAVGCILAELLLRVPFLPGDSDLDQLTRIFETLGTPTEEQWPDM
CSLPDYVTFKSFPGIPLHHIFSAAGDDLLDLIQGLFLFNPCARITATQALKMKYFSNRPG
PTPGCQLPRPNCPVETLKEQSNPALAIKRKRTEALEQGGLPKKLIF
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Component 2 |
Name: | Cyclin-H |
Synonyms: | CCNH | CCNH_HUMAN | Cyclin H | MO15-associated protein | p34 | p37 |
Type: | Enzyme Subunit |
Mol. Mass.: | 37646.05 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 323 |
Sequence: | MYHNSSQKRHWTFSSEEQLARLRADANRKFRCKAVANGKVLPNDPVFLEPHEEMTLCKYY
EKRLLEFCSVFKPAMPRSVVGTACMYFKRFYLNNSVMEYHPRIIMLTCAFLACKVDEFNV
SSPQFVGNLRESPLGQEKALEQILEYELLLIQQLNFHLIVHNPYRPFEGFLIDLKTRYPI
LENPEILRKTADDFLNRIALTDAYLLYTPSQIALTAILSSASRAGITMESYLSESLMLKE
NRTCLSQLLDIMKSMRNLVKKYEPPRSEEVAVLKQKLERCHSAELALNVITKKRKGYEDD
DYVSKKSKHEEEEWTDDDLVESL
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Component 3 |
Name: | CDK-activating kinase assembly factor MAT1 |
Synonyms: | CAP35 | CDK7/cyclin-H assembly factor | Cyclin-G1-interacting protein | MAT1 | MAT1_HUMAN | MNAT1 | Menage a trois | RING finger protein 66 | RING finger protein MAT1 | RNF66 | p35 | p36 |
Type: | Enzyme |
Mol. Mass.: | 35820.03 |
Organism: | Homo sapiens (Human) |
Description: | P51948 |
Residue: | 309 |
Sequence: | MDDQGCPRCKTTKYRNPSLKLMVNVCGHTLCESCVDLLFVRGAGNCPECGTPLRKSNFRV
QLFEDPTVDKEVEIRKKVLKIYNKREEDFPSLREYNDFLEEVEEIVFNLTNNVDLDNTKK
KMEIYQKENKDVIQKNKLKLTREQEELEEALEVERQENEQRRLFIQKEEQLQQILKRKNK
QAFLDELESSDLPVALLLAQHKDRSTQLEMQLEKPKPVKPVTFSTGIKMGQHISLAPIHK
LEEALYEYQPLQIETYGPHVPELEMLGRLGYLNHVRAASPQDLAGGYTSSLACHRALQDA
FSGLFWQPS
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BDBM5655 |
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n/a |
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Name | BDBM5655 |
Synonyms: | 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]-4H-chromen-4-one | CHEMBL428690 | Flavopiridol | US10294218, Example Flavopiridol | US9617225, Flavopiridol |
Type | Small organic molecule |
Emp. Form. | C21H20ClNO5 |
Mol. Mass. | 401.84 |
SMILES | CN1CC[C@@H]([C@H](O)C1)c1c(O)cc(O)c2c1oc(cc2=O)-c1ccccc1Cl |r| |
Structure |
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