Reaction Details |
| Report a problem with these data |
Target | Serine/threonine-protein kinase Chk1 |
---|
Ligand | BDBM50212492 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_447306 (CHEMBL896339) |
---|
IC50 | 5.2±n/a nM |
---|
Citation | Tong, Y; Claiborne, A; Pyzytulinska, M; Tao, ZF; Stewart, KD; Kovar, P; Chen, Z; Credo, RB; Guan, R; Merta, PJ; Zhang, H; Bouska, J; Everitt, EA; Murry, BP; Hickman, D; Stratton, TJ; Wu, J; Rosenberg, SH; Sham, HL; Sowin, TJ; Lin, NH 1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies. Bioorg Med Chem Lett17:3618-23 (2007) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Serine/threonine-protein kinase Chk1 |
---|
Name: | Serine/threonine-protein kinase Chk1 |
Synonyms: | CHEK1 | CHK1 | CHK1 checkpoint homolog | CHK1_HUMAN | Checkpoint kinase-1 (CHK1) |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 54443.02 |
Organism: | Homo sapiens (Human) |
Description: | gi_166295192 |
Residue: | 476 |
Sequence: | MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINK
MLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVY
LHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLK
RREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLA
LLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDF
SPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLL
GTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRR
NNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT
|
|
|
BDBM50212492 |
---|
n/a |
---|
Name | BDBM50212492 |
Synonyms: | 4'-{7-[(2-dimethylamino-ethylamino)-methyl]-1,4-dihydro-indeno[1,2-c]pyrazol-3-yl}-biphenyl-4-ol | CHEMBL234867 |
Type | Small organic molecule |
Emp. Form. | C27H28N4O |
Mol. Mass. | 424.5374 |
SMILES | CN(C)CCNCc1ccc2Cc3c(n[nH]c3-c2c1)-c1ccc(cc1)-c1ccc(O)cc1 |
Structure |
|