Reaction Details |
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Target | Lysine-specific demethylase 3A |
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Ligand | BDBM60875 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1519867 (CHEMBL3624710) |
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IC50 | 39811±n/a nM |
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Citation | England, KS; Tumber, A; Krojer, T; Scozzafava, G; Ng, SS; Daniel, M; Szykowska, A; Che, K; von Delft, F; Burgess-Brown, NA; Kawamura, A; Schofield, CJ; Brennan, PE Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. Medchemcomm5:1879-1886 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Lysine-specific demethylase 3A |
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Name: | Lysine-specific demethylase 3A |
Synonyms: | JHDM2A | JMJD1 | JMJD1A | JmjC domain-containing histone demethylation protein 2A | Jumonji domain-containing protein 1A | KDM3A | KDM3A_HUMAN | KIAA0742 | Lysine-specific demethylase 3A (KDM3A) | TSGA |
Type: | PROTEIN |
Mol. Mass.: | 147368.22 |
Organism: | Homo sapiens (Human) |
Description: | Q9Y4C1 |
Residue: | 1321 |
Sequence: | MVLTLGESWPVLVGRRFLSLSAADGSDGSHDSWDVERVAEWPWLSGTIRAVSHTDVTKKD
LKVCVEFDGESWRKRRWIEVYSLLRRAFLVEHNLVLAERKSPEISERIVQWPAITYKPLL
DKAGLGSITSVRFLGDQQRVFLSKDLLKPIQDVNSLRLSLTDNQIVSKEFQALIVKHLDE
SHLLKGDKNLVGSEVKIYSLDPSTQWFSATVINGNPASKTLQVNCEEIPALKIVDPSLIH
VEVVHDNLVTCGNSARIGAVKRKSSENNGTLVSKQAKSCSEASPSMCPVQSVPTTVFKEI
LLGCTAATPPSKDPRQQSTPQAANSPPNLGAKIPQGCHKQSLPEEISSCLNTKSEALRTK
PDVCKAGLLSKSSQIGTGDLKILTEPKGSCTQPKTNTDQENRLESVPQALTGLPKECLPT
KASSKAELEIANPPELQKHLEHAPSPSDVSNAPEVKAGVNSDSPNNCSGKKVEPSALACR
SQNLKESSVKVDNESCCSRSNNKIQNAPSRKSVLTDPAKLKKLQQSGEAFVQDDSCVNIV
AQLPKCRECRLDSLRKDKEQQKDSPVFCRFFHFRRLQFNKHGVLRVEGFLTPNKYDNEAI
GLWLPLTKNVVGIDLDTAKYILANIGDHFCQMVISEKEAMSTIEPHRQVAWKRAVKGVRE
MCDVCDTTIFNLHWVCPRCGFGVCVDCYRMKRKNCQQGAAYKTFSWLKCVKSQIHEPENL
MPTQIIPGKALYDVGDIVHSVRAKWGIKANCPCSNRQFKLFSKPASKEDLKQTSLAGEKP
TLGAVLQQNPSVLEPAAVGGEAASKPAGSMKPACPASTSPLNWLADLTSGNVNKENKEKQ
PTMPILKNEIKCLPPLPPLSKSSTVLHTFNSTILTPVSNNNSGFLRNLLNSSTGKTENGL
KNTPKILDDIFASLVQNKTTSDLSKRPQGLTIKPSILGFDTPHYWLCDNRLLCLQDPNNK
SNWNVFRECWKQGQPVMVSGVHHKLNSELWKPESFRKEFGEQEVDLVNCRTNEIITGATV
GDFWDGFEDVPNRLKNEKEPMVLKLKDWPPGEDFRDMMPSRFDDLMANIPLPEYTRRDGK
LNLASRLPNYFVRPDLGPKMYNAYGLITPEDRKYGTTNLHLDVSDAANVMVYVGIPKGQC
EQEEEVLKTIQDGDSDELTIKRFIEGKEKPGALWHIYAAKDTEKIREFLKKVSEEQGQEN
PADHDPIHDQSWYLDRSLRKRLHQEYGVQGWAIVQFLGDVVFIPAGAPHQVHNLYSCIKV
AEDFVSPEHVKHCFWLTQEFRYLSQTHTNHEDKLQVKNVIYHAVKDAVAMLKASESSFGK
P
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BDBM60875 |
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n/a |
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Name | BDBM60875 |
Synonyms: | 3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid | 3-{[2-(pyridin-2-yl)-6-(2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl)pyrimidin-4-yl]amino}propanoic acid | GSK J1 | GSK-J1 | GSKJ1 |
Type | n/a |
Emp. Form. | C22H23N5O2 |
Mol. Mass. | 389.4503 |
SMILES | OC(=O)CCNc1cc(nc(n1)-c1ccccn1)N1CCc2ccccc2CC1 |
Structure |
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