Reaction Details |
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Target | Serine/threonine-protein kinase Chk2 |
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Ligand | BDBM2579 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_791991 (CHEMBL1930051) |
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IC50 | 27±n/a nM |
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Citation | Reader, JC; Matthews, TP; Klair, S; Cheung, KM; Scanlon, J; Proisy, N; Addison, G; Ellard, J; Piton, N; Taylor, S; Cherry, M; Fisher, M; Boxall, K; Burns, S; Walton, MI; Westwood, IM; Hayes, A; Eve, P; Valenti, M; de Haven Brandon, A; Box, G; van Montfort, RL; Williams, DH; Aherne, GW; Raynaud, FI; Eccles, SA; Garrett, MD; Collins, I Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem54:8328-42 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase Chk2 |
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Name: | Serine/threonine-protein kinase Chk2 |
Synonyms: | CDS1 | CHEK2 | CHK2 | CHK2_HUMAN | Checkpoint Kinase (Chk2) | RAD53 | Serine/threonine-protein kinase Chek2 | Serine/threonine-protein kinase Chk1/2 |
Type: | Protein |
Mol. Mass.: | 60908.59 |
Organism: | Homo sapiens (Human) |
Description: | O96017 |
Residue: | 543 |
Sequence: | MSRESDVEAQQSHGSSACSQPHGSVTQSQGSSSQSQGISSSSTSTMPNSSQSSHSSSGTL
SSLETVSTQELYSIPEDQEPEDQEPEEPTPAPWARLWALQDGFANLECVNDNYWFGRDKS
CEYCFDEPLLKRTDKYRTYSKKHFRIFREVGPKNSYIAYIEDHSGNGTFVNTELVGKGKR
RPLNNNSEIALSLSRNKVFVFFDLTVDDQSVYPKALRDEYIMSKTLGSGACGEVKLAFER
KTCKKVAIKIISKRKFAIGSAREADPALNVETEIEILKKLNHPCIIKIKNFFDAEDYYIV
LELMEGGELFDKVVGNKRLKEATCKLYFYQMLLAVQYLHENGIIHRDLKPENVLLSSQEE
DCLIKITDFGHSKILGETSLMRTLCGTPTYLAPEVLVSVGTAGYNRAVDCWSLGVILFIC
LSGYPPFSEHRTQVSLKDQITSGKYNFIPEVWAEVSEKALDLVKKLLVVDPKARFTTEEA
LRHPWLQDEDMKRKFQDLLSEENESTALPQVLAQPSTSRKRPREGEAEGAETTKRPAVCA
AVL
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BDBM2579 |
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n/a |
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Name | BDBM2579 |
Synonyms: | (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine |
Type | Small organic molecule |
Emp. Form. | C28H26N4O3 |
Mol. Mass. | 466.531 |
SMILES | CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r| |
Structure |
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