Reaction Details |
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Target | Lysine-specific demethylase 6A |
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Ligand | BDBM60875 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1797930 (CHEMBL4270047) |
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IC50 | 69000±n/a nM |
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Citation | Horton, JR; Woodcock, CB; Chen, Q; Liu, X; Zhang, X; Shanks, J; Rai, G; Mott, BT; Jansen, DJ; Kales, SC; Henderson, MJ; Cyr, M; Pohida, K; Hu, X; Shah, P; Xu, X; Jadhav, A; Maloney, DJ; Hall, MD; Simeonov, A; Fu, H; Vertino, PM; Cheng, X Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A. J Med Chem61:10588-10601 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Lysine-specific demethylase 6A |
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Name: | Lysine-specific demethylase 6A |
Synonyms: | Histone demethylase UTX | KDM6A | KDM6A_HUMAN | Lysine-specific demethylase 6A | Lysine-specific demethylase 6A (KDM6A(UTX)) | Lysine-specific demethylase 6A (KDM6A) | UTX | Ubiquitously-transcribed TPR protein on the X chromosome | Ubiquitously-transcribed X chromosome tetratricopeptide repeat protein |
Type: | Protein |
Mol. Mass.: | 154198.48 |
Organism: | Homo sapiens (Human) |
Description: | O15550 |
Residue: | 1401 |
Sequence: | MKSCGVSLATAAAAAAAFGDEEKKMAAGKASGESEEASPSLTAEEREALGGLDSRLFGFV
RFHEDGARTKALLGKAVRCYESLILKAEGKVESDFFCQLGHFNLLLEDYPKALSAYQRYY
SLQSDYWKNAAFLYGLGLVYFHYNAFQWAIKAFQEVLYVDPSFCRAKEIHLRLGLMFKVN
TDYESSLKHFQLALVDCNPCTLSNAEIQFHIAHLYETQRKYHSAKEAYEQLLQTENLSAQ
VKATVLQQLGWMHHTVDLLGDKATKESYAIQYLQKSLEADPNSGQSWYFLGRCYSSIGKV
QDAFISYRQSIDKSEASADTWCSIGVLYQQQNQPMDALQAYICAVQLDHGHAAAWMDLGT
LYESCNQPQDAIKCYLNATRSKSCSNTSALAARIKYLQAQLCNLPQGSLQNKTKLLPSIE
EAWSLPIPAELTSRQGAMNTAQQNTSDNWSGGHAVSHPPVQQQAHSWCLTPQKLQHLEQL
RANRNNLNPAQKLMLEQLESQFVLMQQHQMRPTGVAQVRSTGIPNGPTADSSLPTNSVSG
QQPQLALTRVPSVSQPGVRPACPGQPLANGPFSAGHVPCSTSRTLGSTDTILIGNNHITG
SGSNGNVPYLQRNALTLPHNRTNLTSSAEEPWKNQLSNSTQGLHKGQSSHSAGPNGERPL
SSTGPSQHLQAAGSGIQNQNGHPTLPSNSVTQGAALNHLSSHTATSGGQQGITLTKESKP
SGNILTVPETSRHTGETPNSTASVEGLPNHVHQMTADAVCSPSHGDSKSPGLLSSDNPQL
SALLMGKANNNVGTGTCDKVNNIHPAVHTKTDNSVASSPSSAISTATPSPKSTEQTTTNS
VTSLNSPHSGLHTINGEGMEESQSPMKTDLLLVNHKPSPQIIPSMSVSIYPSSAEVLKAC
RNLGKNGLSNSSILLDKCPPPRPPSSPYPPLPKDKLNPPTPSIYLENKRDAFFPPLHQFC
TNPNNPVTVIRGLAGALKLDLGLFSTKTLVEANNEHMVEVRTQLLQPADENWDPTGTKKI
WHCESNRSHTTIAKYAQYQASSFQESLREENEKRSHHKDHSDSESTSSDNSGRRRKGPFK
TIKFGTNIDLSDDKKWKLQLHELTKLPAFVRVVSAGNLLSHVGHTILGMNTVQLYMKVPG
SRTPGHQENNNFCSVNINIGPGDCEWFVVPEGYWGVLNDFCEKNNLNFLMGSWWPNLEDL
YEANVPVYRFIQRPGDLVWINAGTVHWVQAIGWCNNIAWNVGPLTACQYKLAVERYEWNK
LQSVKSIVPMVHLSWNMARNIKVSDPKLFEMIKYCLLRTLKQCQTLREALIAAGKEIIWH
GRTKEEPAHYCSICEVEVFDLLFVTNESNSRKTYIVHCQDCARKTSGNLENFVVLEQYKM
EDLMQVYDQFTLAPPLPSASS
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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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