Target
Histone lysine demethylase PHF8
Ligand
BDBM276057
Substrate
n/a
Meas. Tech.
PHF8 Assay
IC50
300±n/a nM
Citation
 Chen, YKNie, ZStafford, JAVeal, 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:
BDBM276057
Synonyms:
2-[1-[(2,3-dichlorophenyl)methyl]imidazol-4-yl]-4-(5-iodo-1H-triazol-4-yl)pyridine | US10071984, Example 19 | US10174003, Example 19 | US9896436, Example 19
Type:
Small organic molecule
Emp. Form.:
C17H11Cl2IN6
Mol. Mass.:
497.12
SMILES:
Clc1cccc(Cn2cnc(c2)-c2cc(ccn2)-c2nn[nH]c2I)c1Cl
Structure:
Search PDB for entries with ligand similarity: