Reaction Details |
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Target | Lysine-specific demethylase 5B |
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Ligand | BDBM50513346 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1853107 (CHEMBL4353731) |
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Ki | 16±n/a nM |
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Citation | Le Bihan, YV; Lanigan, RM; Atrash, B; McLaughlin, MG; Velupillai, S; Malcolm, AG; England, KS; Ruda, GF; Mok, NY; Tumber, A; Tomlin, K; Saville, H; Shehu, E; McAndrew, C; Carmichael, L; Bennett, JM; Jeganathan, F; Eve, P; Donovan, A; Hayes, A; Wood, F; Raynaud, FI; Fedorov, O; Brennan, PE; Burke, R; van Montfort, RLM; Rossanese, OW; Blagg, J; Bavetsias, V C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays. Eur J Med Chem177:316-337 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Lysine-specific demethylase 5B |
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Name: | Lysine-specific demethylase 5B |
Synonyms: | CT31 | Cancer/testis antigen 31 | Histone demethylase JARID1B | JARID1B | Jumonji/ARID domain-containing protein 1B | KDM5B | KDM5B_HUMAN | Lysine-specific demethylase 5B (KDM5B) | Lysine-specific demethylase 5B (KDM5Flag-5B-FL) | PLU-1 | PLU1 | RBBP2H1 | RBP2-H1 | Retinoblastoma-binding protein 2 homolog 1 |
Type: | Protein |
Mol. Mass.: | 175659.67 |
Organism: | Homo sapiens (Human) |
Description: | Q9UGL1 |
Residue: | 1544 |
Sequence: | MEAATTLHPGPRPALPLGGPGPLGEFLPPPECPVFEPSWEEFADPFAFIHKIRPIAEQTG
ICKVRPPPDWQPPFACDVDKLHFTPRIQRLNELEAQTRVKLNFLDQIAKYWELQGSTLKI
PHVERKILDLFQLNKLVAEEGGFAVVCKDRKWTKIATKMGFAPGKAVGSHIRGHYERILN
PYNLFLSGDSLRCLQKPNLTTDTKDKEYKPHDIPQRQSVQPSETCPPARRAKRMRAEAMN
IKIEPEETTEARTHNLRRRMGCPTPKCENEKEMKSSIKQEPIERKDYIVENEKEKPKSRS
KKATNAVDLYVCLLCGSGNDEDRLLLCDGCDDSYHTFCLIPPLHDVPKGDWRCPKCLAQE
CSKPQEAFGFEQAARDYTLRTFGEMADAFKSDYFNMPVHMVPTELVEKEFWRLVSTIEED
VTVEYGADIASKEFGSGFPVRDGKIKLSPEEEEYLDSGWNLNNMPVMEQSVLAHITADIC
GMKLPWLYVGMCFSSFCWHIEDHWSYSINYLHWGEPKTWYGVPGYAAEQLENVMKKLAPE
LFVSQPDLLHQLVTIMNPNTLMTHEVPVYRTNQCAGEFVITFPRAYHSGFNQGFNFAEAV
NFCTVDWLPLGRQCVEHYRLLHRYCVFSHDEMICKMASKADVLDVVVASTVQKDMAIMIE
DEKALRETVRKLGVIDSERMDFELLPDDERQCVKCKTTCFMSAISCSCKPGLLVCLHHVK
ELCSCPPYKYKLRYRYTLDDLYPMMNALKLRAESYNEWALNVNEALEAKINKKKSLVSFK
ALIEESEMKKFPDNDLLRHLRLVTQDAEKCASVAQQLLNGKRQTRYRSGGGKSQNQLTVN
ELRQFVTQLYALPCVLSQTPLLKDLLNRVEDFQQHSQKLLSEETPSAAELQDLLDVSFEF
DVELPQLAEMRIRLEQARWLEEVQQACLDPSSLTLDDMRRLIDLGVGLAPYSAVEKAMAR
LQELLTVSEHWDDKAKSLLKARPRHSLNSLATAVKEIEEIPAYLPNGAALKDSVQRARDW
LQDVEGLQAGGRVPVLDTLIELVTRGRSIPVHLNSLPRLETLVAEVQAWKECAVNTFLTE
NSPYSLLEVLCPRCDIGLLGLKRKQRKLKEPLPNGKKKSTKLESLSDLERALTESKETAS
AMATLGEARLREMEALQSLRLANEGKLLSPLQDVDIKICLCQKAPAAPMIQCELCRDAFH
TSCVAVPSISQGLRIWLCPHCRRSEKPPLEKILPLLASLQRIRVRLPEGDALRYMIERTV
NWQHRAQQLLSSGNLKFVQDRVGSGLLYSRWQASAGQVSDTNKVSQPPGTTSFSLPDDWD
NRTSYLHSPFSTGRSCIPLHGVSPEVNELLMEAQLLQVSLPEIQELYQTLLAKPSPAQQT
DRSSPVRPSSEKNDCCRGKRDGINSLERKLKRRLEREGLSSERWERVKKMRTPKKKKIKL
SHPKDMNNFKLERERSYELVRSAETHSLPSDTSYSEQEDSEDEDAICPAVSCLQPEGDEV
DWVQCDGSCNQWFHQVCVGVSPEMAEKEDYICVRCTVKDAPSRK
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BDBM50513346 |
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n/a |
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Name | BDBM50513346 |
Synonyms: | CHEMBL4525269 |
Type | Small organic molecule |
Emp. Form. | C20H24N6O |
Mol. Mass. | 364.4442 |
SMILES | O=c1[nH]cnc2c(nccc12)-n1cc(cn1)C1CCN(CC2CCC2)CC1 |
Structure |
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