Reaction Details |
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Target | Lysine-specific demethylase 6A |
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Ligand | BDBM281138 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1685362 |
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IC50 | >25000±n/a nM |
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Citation | Liang, J; Labadie, S; Zhang, B; Ortwine, DF; Patel, S; Vinogradova, M; Kiefer, JR; Mauer, T; Gehling, VS; Harmange, JC; Cummings, R; Lai, T; Liao, J; Zheng, X; Liu, Y; Gustafson, A; Van der Porten, E; Mao, W; Liederer, BM; Deshmukh, G; An, L; Ran, Y; Classon, M; Trojer, P; Dragovich, PS; Murray, L From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors. Bioorg Med Chem Lett27:2974-2981 (2017) [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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BDBM281138 |
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n/a |
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Name | BDBM281138 |
Synonyms: | US10022354, Example 78 |
Type | Small organic molecule |
Emp. Form. | C21H26N6O |
Mol. Mass. | 378.4707 |
SMILES | CC(C)c1cc([nH]n1)C(=O)N1CCC(C1)c1cc(cc(C)n1)-c1cnn(C)c1 |
Structure |
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