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Target
Isoform 2 of Histone lysine demethylase PHF8 (2)
Ligand
BDBM276092
Substrate
n/a
Meas. Tech.
PHF8 Assay
Temperature
298.15±n/a K
IC50
5500±n/a nM
Comments
extracted
Citation
 Chen, YK; Nie, Z; Stafford, JA; Veal, JM Histone demethylase inhibitors US Patent  US10071984 Publication Date 9/11/2018 
Target
Name:
Isoform 2 of Histone lysine demethylase PHF8 (2)
Synonyms:
Histone lysine demethylase PHF8 (2) | KIAA1111 | NP_055922 | PHF8 | PHF8_HUMAN | ZNF422 | histone lysine demethylase PHF8 isoform 2
Type:
Enzyme Catalytic Domain
Mol. Mass.:
113932.27
Organism:
Homo sapiens (Human)
Description:
Q9UPP1-2
Residue:
1024
Sequence:
MASVPVYCLCRLPYDVTRFMIECDMCQDWFHGSCVGVEEEKAADIDLYHCPNCEVLHGPSIMKKRRGSSKGHDTHKGKPVKTGSPTFVRELRSRTFDSSDEVILKPTGNQLTVEFLEENSFSVPILVLKKDGLGMTLPSPSFTVRDVEHYVGSDKEIDVIDVTRQADCKMKLGDFVKYYYSGKREKVLNVISLEFSDTRLSNLVETPKIVRKLSWVENLWPEECVFERPNVQKYCLMSVRDSYTDFHIDFGGTSVWYHVLKGEKIFYLIRPTNANLTLFECWSSSSNQNEMFFGDQVDKCYKCSVKQGQTLFIPTGWIHAVLTPVDCLAFGGNFLHSLNIEMQLKAYEIEKRLSTADLFRFPNFETICWYVGKHILDIFRGLRENRRHPASYLVHGGKALNLAFRAWTRKEALPDHEDEIPETVRTVQLIKDLAREIRLVEDIFQQNVGKTSNIFGLQRIFPAGSIPLTRPAHSTSVSMSRLSLPSKNGSKKKGLKPKELFKKAERKGKESSALGPAGQLSYNLMDTYSHQALKTGSFQKAKFNITGACLNDSDDDSPDLDLDGNESPLALLMSNGSTKRVKSLSKSRRTKIAKKVDKARLMAEQVMEDEFDLDSDDELQIDERLGKEKATLIIRPKFPRKLPRAKPCSDPNRVREPGEVEFDIEEDYTTDEDMVEGVEGKLGNGSGAGGILDLLKASRQVGGPDYAALTEAPASPSTQEAIQGMLCMANLQSSSSSPATSSLQAWWTGGQDRSSGSSSSGLGTVSNSPASQRTPGKRPIKRPAYWRTESEEEEENASLDEQDSLGACFKDAEYIYPSLESDDDDPALKSRPKKKKNSDDAPWSPKARVTPTLPKQDRPVREGTRVASIETGLAAAAAKLAQQELQKAQKKKYIKKKPLLKEVEQPRPQDSNLSLTVPAPTVAATPQLVTSSSPLPPPEPKQEALSGSLADHEYTARPNAFGMAQANRSTTPMAPGVFLTQRRPSVGSQSNQAGQGKRPKKGLATAKQRLGRILKIHRNGKLLL
  
Inhibitor
Name:
BDBM276092
Synonyms:
5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methyl-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole | US10071984, Example 54 | US10174003, Example 54 | US9896436, Example 54
Type:
Small organic molecule
Emp. Form.:
C19H17FN6O
Mol. Mass.:
364.3763
SMILES:
Cn1cnc(c1-c1ccc(F)cc1OCC1CC1)-c1cc2[nH]nnc2cn1 |(2.41,-2.3,;.92,-2.7,;.45,-4.16,;-1.09,-4.16,;-1.57,-2.7,;-.32,-1.79,;.07,-.3,;-1.01,.79,;-.62,2.27,;.87,2.67,;1.27,4.16,;1.96,1.58,;1.56,.1,;2.65,-.99,;4.14,-.59,;5.23,-1.68,;5.63,-3.17,;6.72,-2.08,;-2.9,-1.93,;-2.9,-.39,;-4.24,.38,;-4.56,1.89,;-6.09,2.05,;-6.72,.65,;-5.57,-.39,;-5.57,-1.93,;-4.24,-2.7,)|
Structure:
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