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Target
Cyclin-H/Cyclin-dependent kinase 7
Ligand
BDBM12121
Substrate
FAM-CDK7 derived peptide
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
IC50
25±n/a nM
Citation
Fraley, ME; Steen, JT; Brnardic, EJ; Arrington, KL; Spencer, KL; Hanney, BA; Kim, Y; Hartman, GD; Stirdivant, SM; Drakas, BA; Rickert, K; Walsh, ES; Hamilton, K; Buser, CA; Hardwick, J; Tao, W; Beck, SC; Mao, X; Lobell, RB; Sepp-Lorenzino, L; Yan, Y; Ikuta, M; Munshi, SK; Kuo, LC; Kreatsoulas, C 3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6. Bioorg Med Chem Lett 16:6049-53 (2006) [PubMed] Article
More Info.:
Target
Name:
Cyclin-H/Cyclin-dependent kinase 7
Synonyms:
CDK-activating kinase assembly factor MAT1/Cyclin H/Cyclin-dependent kinase 7 | CDK7/Cyclin H | CDK7/H | Cyclin H/dependent kinase 7 | Cyclin-Dependent Kinase 7 (CDK7) | Cyclin-dependent kinase 7/ cyclin H | Cyclin-dependent kinase 7/cyclin H
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-H
Synonyms:
CCNH | CCNH_HUMAN | Cyclin H | MO15-associated protein | p34 | p37
Type:
Enzyme Subunit
Mol. Mass.:
37646.05
Organism:
Human
Description:
n/a
Residue:
323
Sequence:
MYHNSSQKRHWTFSSEEQLARLRADANRKFRCKAVANGKVLPNDPVFLEPHEEMTLCKYYEKRLLEFCSVFKPAMPRSVVGTACMYFKRFYLNNSVMEYHPRIIMLTCAFLACKVDEFNVSSPQFVGNLRESPLGQEKALEQILEYELLLIQQLNFHLIVHNPYRPFEGFLIDLKTRYPILENPEILRKTADDFLNRIALTDAYLLYTPSQIALTAILSSASRAGITMESYLSESLMLKENRTCLSQLLDIMKSMRNLVKKYEPPRSEEVAVLKQKLERCHSAELALNVITKKRKGYEDDDYVSKKSKHEEEEWTDDDLVESL
Component 2
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:
Human
Description:
n/a
Residue:
346
Sequence:
MALDVKSRAKRYEKLDFLGEGQFATVYKARDKNTNQIVAIKKIKLGHRSEAKDGINRTALREIKLLQELSHPNIIGLLDAFGHKSNISLVFDFMETDLEVIIKDNSLVLTPSHIKAYMLMTLQGLEYLHQHWILHRDLKPNNLLLDENGVLKLADFGLAKSFGSPNRAYTHQVVTRWYRAPELLFGARMYGVGVDMWAVGCILAELLLRVPFLPGDSDLDQLTRIFETLGTPTEEQWPDMCSLPDYVTFKSFPGIPLHHIFSAAGDDLLDLIQGLFLFNPCARITATQALKMKYFSNRPGPTPGCQLPRPNCPVETLKEQSNPALAIKRKRTEALEQGGLPKKLIF
Inhibitor
Name:
BDBM12121
Synonyms:
3-(Indol-2-yl)indazole 11 | 4-({2-[6-(1H-pyrazol-4-yl)-1H-indazol-3-yl]-1H-indol-5-yl}methyl)morpholine
Type:
Small organic molecule
Emp. Form.:
C23H22N6O
Mol. Mass.:
398.4604
SMILES:
C(N1CCOCC1)c1ccc2[nH]c(cc2c1)-c1n[nH]c2cc(ccc12)-c1cn[nH]c1
Substrate
Name:
FAM-CDK7 derived peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2205.10
Organism:
n/a
Description:
n/a
Residue:
19
Sequence:
FAMFLAKSFGSPNRAYKKH