Reaction Details |
| Report a problem with these data |
Target | Lysine-specific demethylase 5B |
---|
Ligand | BDBM264001 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1771179 (CHEMBL4223291) |
---|
IC50 | 4.0±n/a nM |
---|
Citation | Nie, Z; Shi, L; Lai, C; O'Connell, SM; Xu, J; Stansfield, RK; Hosfield, DJ; Veal, JM; Stafford, JA Structure-based design and discovery of potent and selective KDM5 inhibitors. Bioorg Med Chem Lett28:1490-1494 (2018) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Lysine-specific demethylase 5B |
---|
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
|
|
|
BDBM264001 |
---|
n/a |
---|
Name | BDBM264001 |
Synonyms: | 2-{5-[(4-chloro-2- fluorobenzyl)oxy]-1H-pyrazol-1- yl}pyridine-4-carboxylic acid | US10173996, Example 75 | US9604961, Example 75 | US9714230, 75 | US9908865, Example 75 |
Type | Small organic molecule |
Emp. Form. | C16H11ClFN3O3 |
Mol. Mass. | 347.728 |
SMILES | OC(=O)c1ccnc(c1)-n1nccc1OCc1ccc(Cl)cc1F |
Structure |
|