Reaction Details |
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Target | Lysine-specific demethylase 5C |
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Ligand | BDBM50153099 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1561972 |
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IC50 | 24±n/a nM |
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Citation | Bavetsias V; Lanigan RM; Ruda GF; Atrash B; McLaughlin MG; Tumber A; Mok NY; Le Bihan YV; Dempster S; Boxall KJ; Jeganathan F; Hatch SB; Savitsky P; Velupillai S; Krojer T; England KS; Sejberg J; Thai C; Donovan A; Pal A; Scozzafava G; Bennett JM; Kawamura A; Johansson C; Szykowska A; Gileadi C; Burgess-Brown NA; von Delft F; Oppermann U; Walters Z; Shipley J; Raynaud FI; Westaway SM; Prinjha RK; Fedorov O; Burke R; Schofield CJ; Westwood IM; Bountra C; Müller S; van Montfort RL; Brennan PE; Blagg J 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. J Med Chem 59:1388-409 (2016) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Lysine-specific demethylase 5C |
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Name: | Lysine-specific demethylase 5C |
Synonyms: | DXS1272E | Histone demethylase JARID1C | JARID1C | Jumonji/ARID domain-containing protein 1C | KDM5C | Lysine-specific demethylase 5C (KDM5C) | Lysine-specific demethylase 5C (KDM5Flag-5C-FL) | Protein SmcX | Protein Xe169 | SMCX | XE169 |
Type: | PROTEIN |
Mol. Mass.: | 175691.17 |
Organism: | Homo sapiens (Human) |
Description: | P41229 |
Residue: | 1560 |
Sequence: | MEPGSDDFLPPPECPVFEPSWAEFRDPLGYIAKIRPIAEKSGICKIRPPADWQPPFAVEV
DNFRFTPRIQRLNELEAQTRVKLNYLDQIAKFWEIQGSSLKIPNVERRILDLYSLSKIVV
EEGGYEAICKDRRWARVAQRLNYPPGKNIGSLLRSHYERIVYPYEMYQSGANLVQCNTRP
FDNEEKDKEYKPHSIPLRQSVQPSKFNSYGRRAKRLQPDPEPTEEDIEKNPELKKLQIYG
AGPKMMGLGLMAKDKTLRKKDKEGPECPPTVVVKEELGGDVKVESTSPKTFLESKEELSH
SPEPCTKMTMRLRRNHSNAQFIESYVCRMCSRGDEDDKLLLCDGCDDNYHIFCLLPPLPE
IPKGVWRCPKCVMAECKRPPEAFGFEQATREYTLQSFGEMADSFKADYFNMPVHMVPTEL
VEKEFWRLVNSIEEDVTVEYGADIHSKEFGSGFPVSDSKRHLTPEEEEYATSGWNLNVMP
VLEQSVLCHINADISGMKVPWLYVGMVFSAFCWHIEDHWSYSINYLHWGEPKTWYGVPSL
AAEHLEEVMKKLTPELFDSQPDLLHQLVTLMNPNTLMSHGVPVVRTNQCAGEFVITFPRA
YHSGFNQGYNFAEAVNFCTADWLPAGRQCIEHYRRLRRYCVFSHEELICKMAACPEKLDL
NLAAAVHKEMFIMVQEERRLRKALLEKGITEAEREAFELLPDDERQCIKCKTTCFLSALA
CYDCPDGLVCLSHINDLCKCSSSRQYLRYRYTLDELPAMLHKLKVRAESFDTWANKVRVA
LEVEDGRKRSLEELRALESEARERRFPNSELLQQLKNCLSEAEACVSRALGLVSGQEAGP
HRVAGLQMTLTELRAFLDQMNNLPCAMHQIGDVKGVLEQVEAYQAEAREALASLPSSPGL
LQSLLERGRQLGVEVPEAQQLQRQVEQARWLDEVKRTLAPSARRGTLAVMRGLLVAGASV
APSPAVDKAQAELQELLTIAERWEEKAHLCLEARQKHPPATLEAIIREAENIPVHLPNIQ
ALKEALAKARAWIADVDEIQNGDHYPCLDDLEGLVAVGRDLPVGLEELRQLELQVLTAHS
WREKASKTFLKKNSCYTLLEVLCPCADAGSDSTKRSRWMEKELGLYKSDTELLGLSAQDL
RDPGSVIVAFKEGEQKEKEGILQLRRTNSAKPSPLASSSTASSTTSICVCGQVLAGAGAL
QCDLCQDWFHGRCVSVPRLLSSPRPNPTSSPLLAWWEWDTKFLCPLCMRSRRPRLETILA
LLVALQRLPVRLPEGEALQCLTERAISWQGRARQALASEDVTALLGRLAELRQRLQAEPR
PEEPPNYPAAPASDPLREGSGKDMPKVQGLLENGDSVTSPEKVAPEEGSGKRDLELLSSL
LPQLTGPVLELPEATRAPLEELMMEGDLLEVTLDENHSIWQLLQAGQPPDLERIRTLLEL
EKAERHGSRARGRALERRRRRKVDRGGEGDDPAREELEPKRVRSSGPEAEEVQEEEELEE
ETGGEGPPAPIPTTGSPSTQENQNGLEPAEGTTSGPSAPFSTLTPRLHLPCPQQPPQQQL
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BDBM50153099 |
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n/a |
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Name | BDBM50153099 |
Synonyms: | CHEMBL3775814 |
Type | Small organic molecule |
Emp. Form. | C24H23N7O |
Mol. Mass. | 425.4857 |
SMILES | O=c1[nH]cnc2c(nccc12)-n1cc(CCN2CCC(CC2)c2ccc(cc2)C#N)cn1 |
Structure |
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