Reaction Details |
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Target | Histone acetyltransferase KAT6A [507-778] |
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Ligand | BDBM50518832 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1873647 (CHEMBL4374936) |
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IC50 | 8.0±n/a nM |
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Citation | Leaver, DJ; Cleary, B; Nguyen, N; Priebbenow, DL; Lagiakos, HR; Sanchez, J; Xue, L; Huang, F; Sun, Y; Mujumdar, P; Mudududdla, R; Varghese, S; Teguh, S; Charman, SA; White, KL; Katneni, K; Cuellar, M; Strasser, JM; Dahlin, JL; Walters, MA; Street, IP; Monahan, BJ; Jarman, KE; Sabroux, HJ; Falk, H; Chung, MC; Hermans, SJ; Parker, MW; Thomas, T; Baell, JB Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A. J Med Chem62:7146-7159 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone acetyltransferase KAT6A [507-778] |
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Name: | Histone acetyltransferase KAT6A [507-778] |
Synonyms: | 2.3.1.48 | Histone acetyltransferase KAT6A | KAT6A | KAT6A_HUMAN | MOZ | MOZ, YBF2/SAS3, SAS2 and TIP60 protein 3 | MYST-3 | MYST3 | Monocytic leukemia zinc finger protein | RUNXBP2 | Runt-related transcription factor-binding protein 2 | ZNF220 | Zinc finger protein 220 |
Type: | PROTEIN |
Mol. Mass.: | 224994.11 |
Organism: | Homo sapiens |
Description: | Q92794[507-778] |
Residue: | 2004 |
Sequence: | MVKLANPLYTEWILEAIKKVKKQKQRPSEERICNAVSSSHGLDRKTVLEQLELSVKDGTI
LKVSNKGLNSYKDPDNPGRIALPKPRNHGKLDNKQNVDWNKLIKRAVEGLAESGGSTLKS
IERFLKGQKDVSALFGGSAASGFHQQLRLAIKRAIGHGRLLKDGPLYRLNTKATNVDGKE
SCESLSCLPPVSLLPHEKDKPVAEPIPICSFCLGTKEQNREKKPEELISCADCGNSGHPS
CLKFSPELTVRVKALRWQCIECKTCSSCRDQGKNADNMLFCDSCDRGFHMECCDPPLTRM
PKGMWICQICRPRKKGRKLLQKKAAQIKRRYTNPIGRPKNRLKKQNTVSKGPFSKVRTGP
GRGRKRKITLSSQSASSSSEEGYLERIDGLDFCRDSNVSLKFNKKTKGLIDGLTKFFTPS
PDGRKARGEVVDYSEQYRIRKRGNRKSSTSDWPTDNQDGWDGKQENEERLFGSQEIMTEK
DMELFRDIQEQALQKVGVTGPPDPQVRCPSVIEFGKYEIHTWYSSPYPQEYSRLPKLYLC
EFCLKYMKSRTILQQHMKKCGWFHPPANEIYRKNNISVFEVDGNVSTIYCQNLCLLAKLF
LDHKTLYYDVEPFLFYVLTQNDVKGCHLVGYFSKEKHCQQKYNVSCIMILPQYQRKGYGR
FLIDFSYLLSKREGQAGSPEKPLSDLGRLSYMAYWKSVILECLYHQNDKQISIKKLSKLT
GICPQDITSTLHHLRMLDFRSDQFVIIRREKLIQDHMAKLQLNLRPVDVDPECLRWTPVI
VSNSVVSEEEEEEAEEGENEEPQCQERELEISVGKSVSHENKEQDSYSVESEKKPEVMAP
VSSTRLSKQVLPHDSLPANSQPSRRGRWGRKNRKTQERFGDKDSKLLLEETSSAPQEQYG
ECGEKSEATQEQYTESEEQLVASEEQPSQDGKPDLPKRRLSEGVEPWRGQLKKSPEALKC
RLTEGSERLPRRYSEGDRAVLRGFSESSEEEEEPESPRSSSPPILTKPTLKRKKPFLHRR
RRVRKRKHHNSSVVTETISETTEVLDEPFEDSDSERPMPRLEPTFEIDEEEEEEDENELF
PREYFRRLSSQDVLRCQSSSKRKSKDEEEDEESDDADDTPILKPVSLLRKRDVKNSPLEP
DTSTPLKKKKGWPKGKSRKPIHWKKRPGRKPGFKLSREIMPVSTQACVIEPIVSIPKAGR
KPKIQESEETVEPKEDMPLPEERKEEEEMQAEAEEAEEGEEEDAASSEVPAASPADSSNS
PETETKEPEVEEEEEKPRVSEEQRQSEEEQQELEEPEPEEEEDAAAETAQNDDHDADDED
DGHLESTKKKELEEQPTREDVKEEPGVQESFLDANMQKSREKIKDKEETELDSEEEQPSH
DTSVVSEQMAGSEDDHEEDSHTKEELIELKEEEEIPHSELDLETVQAVQSLTQEESSEHE
GAYQDCEETLAACQTLQSYTQADEDPQMSMVEDCHASEHNSPISSVQSHPSQSVRSVSSP
NVPALESGYTQISPEQGSLSAPSMQNMETSPMMDVPSVSDHSQQVVDSGFSDLGSIESTT
ENYENPSSYDSTMGGSICGNSSSQSSCSYGGLSSSSSLTQSSCVVTQQMASMGSSCSMMQ
QSSVQPAANCSIKSPQSCVVERPPSNQQQQPPPPPPQQPQPPPPQPQPAPQPPPPQQQPQ
QQPQPQPQQPPPPPPPQQQPPLSQCSMNNSFTPAPMIMEIPESGSTGNISIYERIPGDFG
AGSYSQPSATFSLAKLQQLTNTIMDPHAMPYSHSPAVTSYATSVSLSNTGLAQLAPSHPL
AGTPQAQATMTPPPNLASTTMNLTSPLLQCNMSATNIGIPHTQRLQGQMPVKGHISIRSK
SAPLPSAAAHQQQLYGRSPSAVAMQAGPRALAVQRGMNMGVNLMPTPAYNVNSMNMNTLN
AMNSYRMTQPMMNSSYHSNPAYMNQTAQYPMQMQMGMMGSQAYTQQPMQPNPHGNMMYTG
PSHHSYMNAAGVPKQSLNGPYMRR
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BDBM50518832 |
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n/a |
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Name | BDBM50518832 |
Synonyms: | CHEMBL4455897 | US10829446, Compound 36 |
Type | Small organic molecule |
Emp. Form. | C20H17FN2O3S |
Mol. Mass. | 384.424 |
SMILES | Cc1cc(cc(C(=O)NNS(=O)(=O)c2ccccc2)c1F)-c1ccccc1 |
Structure |
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