Reaction Details  Report a problem with these data
Target
Histone lysine demethylase PHF8
Ligand
BDBM276042
Substrate
n/a
Meas. Tech.
PHF8 Assay
IC50
>500±n/a nM
Citation
 Chen, YK; Nie, Z; Stafford, JA; Veal, JM Histone demethylase inhibitors US Patent  US9896436 Publication Date 2/20/2018
Target
Name:
Histone lysine demethylase PHF8
Synonyms:
Histone lysine demethylase PHF8 | Histone lysine demethylase PHF8 (PHF8) | KIAA1111 | Lysine-specific demethylase 7A/7B | PHD finger protein 8 | PHF8 | PHF8_HUMAN | ZNF422
Type:
Protein
Mol. Mass.:
117889.91
Organism:
Homo sapiens (Human)
Description:
Q9UPP1
Residue:
1060
Sequence:
MNRSRAIVQRGRVLPPPAPLDTTNLAGRRTLQGRAKMASVPVYCLCRLPYDVTRFMIECDMCQDWFHGSCVGVEEEKAADIDLYHCPNCEVLHGPSIMKKRRGSSKGHDTHKGKPVKTGSPTFVRELRSRTFDSSDEVILKPTGNQLTVEFLEENSFSVPILVLKKDGLGMTLPSPSFTVRDVEHYVGSDKEIDVIDVTRQADCKMKLGDFVKYYYSGKREKVLNVISLEFSDTRLSNLVETPKIVRKLSWVENLWPEECVFERPNVQKYCLMSVRDSYTDFHIDFGGTSVWYHVLKGEKIFYLIRPTNANLTLFECWSSSSNQNEMFFGDQVDKCYKCSVKQGQTLFIPTGWIHAVLTPVDCLAFGGNFLHSLNIEMQLKAYEIEKRLSTADLFRFPNFETICWYVGKHILDIFRGLRENRRHPASYLVHGGKALNLAFRAWTRKEALPDHEDEIPETVRTVQLIKDLAREIRLVEDIFQQNVGKTSNIFGLQRIFPAGSIPLTRPAHSTSVSMSRLSLPSKNGSKKKGLKPKELFKKAERKGKESSALGPAGQLSYNLMDTYSHQALKTGSFQKAKFNITGACLNDSDDDSPDLDLDGNESPLALLMSNGSTKRVKSLSKSRRTKIAKKVDKARLMAEQVMEDEFDLDSDDELQIDERLGKEKATLIIRPKFPRKLPRAKPCSDPNRVREPGEVEFDIEEDYTTDEDMVEGVEGKLGNGSGAGGILDLLKASRQVGGPDYAALTEAPASPSTQEAIQGMLCMANLQSSSSSPATSSLQAWWTGGQDRSSGSSSSGLGTVSNSPASQRTPGKRPIKRPAYWRTESEEEEENASLDEQDSLGACFKDAEYIYPSLESDDDDPALKSRPKKKKNSDDAPWSPKARVTPTLPKQDRPVREGTRVASIETGLAAAAAKLAQQELQKAQKKKYIKKKPLLKEVEQPRPQDSNLSLTVPAPTVAATPQLVTSSSPLPPPEPKQEALSGSLADHEYTARPNAFGMAQANRSTTPMAPGVFLTQRRPSVGSQSNQAGQGKRPKKGLATAKQRLGRILKIHRNGKLLL
  
Inhibitor
Name:
BDBM276042
Synonyms:
2-[5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methylimidazol-4-yl]-4-(1H-triazol-4-yl)pyridine | US10071984, Example 4 | US10174003, Example 4 | US9896436, Example 4
Type:
Small organic molecule
Emp. Form.:
C21H19FN6O
Mol. Mass.:
390.4136
SMILES:
Cn1cnc(c1-c1ccc(F)cc1OCC1CC1)-c1cc(ccn1)-c1c[nH]nn1 |(1.71,-3.53,;.22,-3.92,;-.68,-5.17,;-2.15,-4.69,;-2.15,-3.15,;-.68,-2.68,;-.29,-1.19,;-1.37,-.1,;-.98,1.39,;.51,1.78,;.91,3.27,;1.6,.7,;1.2,-.79,;2.29,-1.88,;3.78,-1.48,;4.87,-2.57,;5.27,-4.06,;6.36,-2.97,;-3.48,-2.38,;-3.48,-.84,;-4.82,-.07,;-6.15,-.84,;-6.15,-2.38,;-4.82,-3.15,;-4.82,1.47,;-6.06,2.37,;-5.59,3.84,;-4.05,3.84,;-3.57,2.37,)|
Structure:
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