| Reaction Details |
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 | Report a problem with these data |
| Target | PAS domain-containing serine/threonine-protein kinase |
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| Ligand | BDBM50154943 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1562265 (CHEMBL3776910) |
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| IC50 | 260±n/a nM |
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| Citation |  Schiemann, K; Mallinger, A; Wienke, D; Esdar, C; Poeschke, O; Busch, M; Rohdich, F; Eccles, SA; Schneider, R; Raynaud, FI; Czodrowski, P; Musil, D; Schwarz, D; Urbahns, K; Blagg, J Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore. Bioorg Med Chem Lett26:1443-51 (2016) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| PAS domain-containing serine/threonine-protein kinase |
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| Name: | PAS domain-containing serine/threonine-protein kinase |
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| Synonyms: | KIAA0135 | PAS-kinase | PASK | PASKIN | PASK_HUMAN | hPASK |
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| Type: | PROTEIN |
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| Mol. Mass.: | 142867.26 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_944230 |
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| Residue: | 1323 |
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| Sequence: | MEDGGLTAFEEDQRCLSQSLPLPVSAEGPAAQTTAEPSRSFSSAHRHLSRRNGLSRLCQS
RTALSEDRWSSYCLSSLAAQNICTSKLHCPAAPEHTDPSEPRGSVSCCSLLRGLSSGWSS
PLLPAPVCNPNKAIFTVDAKTTEILVANDKACGLLGYSSQDLIGQKLTQFFLRSDSDVVE
ALSEEHMEADGHAAVVFGTVVDIISRSGEKIPVSVWMKRMRQERRLCCVVVLEPVERVST
WVAFQSDGTVTSCDSLFAHLHGYVSGEDVAGQHITDLIPSVQLPPSGQHIPKNLKIQRSV
GRARDGTTFPLSLKLKSQPSSEEATTGEAAPVSGYRASVWVFCTISGLITLLPDGTIHGI
NHSFALTLFGYGKTELLGKNITFLIPGFYSYMDLAYNSSLQLPDLASCLDVGNESGCGER
TLDPWQGQDPAEGGQDPRINVVLAGGHVVPRDEIRKLMESQDIFTGTQTELIAGGQLLSC
LSPQPAPGVDNVPEGSLPVHGEQALPKDQQITALGREEPVAIESPGQDLLGESRSEPVDV
KPFASCEDSEAPVPAEDGGSDAGMCGLCQKAQLERMGVSGPSGSDLWAGAAVAKPQAKGQ
LAGGSLLMHCPCYGSEWGLWWRSQDLAPSPSGMAGLSFGTPTLDEPWLGVENDREELQTC
LIKEQLSQLSLAGALDVPHAELVPTECQAVTAPVSSCDLGGRDLCGGCTGSSSACYALAT
DLPGGLEAVEAQEVDVNSFSWNLKELFFSDQTDQTSSNCSCATSELRETPSSLAVGSDPD
VGSLQEQGSCVLDDRELLLLTGTCVDLGQGRRFRESCVGHDPTEPLEVCLVSSEHYAASD
RESPGHVPSTLDAGPEDTCPSAEEPRLNVQVTSTPVIVMRGAAGLQREIQEGAYSGSCYH
RDGLRLSIQFEVRRVELQGPTPLFCCWLVKDLLHSQRDSAARTRLFLASLPGSTHSTAAE
LTGPSLVEVLRARPWFEEPPKAVELEGLAACEGEYSQKYSTMSPLGSGAFGFVWTAVDKE
KNKEVVVKFIKKEKVLEDCWIEDPKLGKVTLEIAILSRVEHANIIKVLDIFENQGFFQLV
MEKHGSGLDLFAFIDRHPRLDEPLASYIFRQLVSAVGYLRLKDIIHRDIKDENIVIAEDF
TIKLIDFGSAAYLERGKLFYTFCGTIEYCAPEVLMGNPYRGPELEMWSLGVTLYTLVFEE
NPFCELEETVEAAIHPPYLVSKELMSLVSGLLQPVPERRTTLEKLVTDPWVTQPVNLADY
TWEEVFRVNKPESGVLSAASLEMGNRSLSDVAQAQELCGGPVPGEAPNGQGCLHPGDPRL
LTS
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| BDBM50154943 |
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| n/a |
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| Name | BDBM50154943 |
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| Synonyms: | CHEMBL3775576 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H17N5O |
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| Mol. Mass. | 319.3605 |
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| SMILES | CNC(=O)c1ccc2[nH]nc(Cc3ccc4n(C)ncc4c3)c2c1 |
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| Structure | 
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