| Reaction Details |
|---|
 | Report a problem with these data |
| Target | CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7 |
|---|
| Ligand | BDBM144315 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_2106555 (CHEMBL4815230) |
|---|
| Ki | >5000±n/a nM |
|---|
| Citation |  Long, Y; Yu, M; Ochnik, AM; Karanjia, JD; Basnet, SK; Kebede, AA; Kou, L; Wang, S Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations. Eur J Med Chem213:0 (2021) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| CDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7 |
|---|
| 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
|
|
|
|---|
| 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
|
|
|
|---|
| 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
|
|
|
|---|
| BDBM144315 |
|---|
| n/a |
|---|
| Name | BDBM144315 |
|---|
| Synonyms: | Gilteritinib | US11512074, Example T-9 | US8969336, 547 | US8969336, 577 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C29H44N8O3 |
|---|
| Mol. Mass. | 552.7115 |
|---|
| SMILES | CCc1nc(C(N)=O)c(Nc2ccc(N3CCC(CC3)N3CCN(C)CC3)c(OC)c2)nc1NC1CCOCC1 |
|---|
| Structure | 
|
|---|
Search and Browse
