Ki Summary

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Target

Isoform 2 of Histone lysine demethylase PHF8 (2)

Ligand

BDBM276077

Substrate/Competitor

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

More Info.:

Get all data from this article, Assay Method

Isoform 2 of Histone lysine demethylase PHF8 (2)

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:

MASVPVYCLCRLPYDVTRFMIECDMCQDWFHGSCVGVEEEKAADIDLYHCPNCEVLHGPS
IMKKRRGSSKGHDTHKGKPVKTGSPTFVRELRSRTFDSSDEVILKPTGNQLTVEFLEENS
FSVPILVLKKDGLGMTLPSPSFTVRDVEHYVGSDKEIDVIDVTRQADCKMKLGDFVKYYY
SGKREKVLNVISLEFSDTRLSNLVETPKIVRKLSWVENLWPEECVFERPNVQKYCLMSVR
DSYTDFHIDFGGTSVWYHVLKGEKIFYLIRPTNANLTLFECWSSSSNQNEMFFGDQVDKC
YKCSVKQGQTLFIPTGWIHAVLTPVDCLAFGGNFLHSLNIEMQLKAYEIEKRLSTADLFR
FPNFETICWYVGKHILDIFRGLRENRRHPASYLVHGGKALNLAFRAWTRKEALPDHEDEI
PETVRTVQLIKDLAREIRLVEDIFQQNVGKTSNIFGLQRIFPAGSIPLTRPAHSTSVSMS
RLSLPSKNGSKKKGLKPKELFKKAERKGKESSALGPAGQLSYNLMDTYSHQALKTGSFQK
AKFNITGACLNDSDDDSPDLDLDGNESPLALLMSNGSTKRVKSLSKSRRTKIAKKVDKAR
LMAEQVMEDEFDLDSDDELQIDERLGKEKATLIIRPKFPRKLPRAKPCSDPNRVREPGEV
EFDIEEDYTTDEDMVEGVEGKLGNGSGAGGILDLLKASRQVGGPDYAALTEAPASPSTQE
AIQGMLCMANLQSSSSSPATSSLQAWWTGGQDRSSGSSSSGLGTVSNSPASQRTPGKRPI
KRPAYWRTESEEEEENASLDEQDSLGACFKDAEYIYPSLESDDDDPALKSRPKKKKNSDD
APWSPKARVTPTLPKQDRPVREGTRVASIETGLAAAAAKLAQQELQKAQKKKYIKKKPLL
KEVEQPRPQDSNLSLTVPAPTVAATPQLVTSSSPLPPPEPKQEALSGSLADHEYTARPNA
FGMAQANRSTTPMAPGVFLTQRRPSVGSQSNQAGQGKRPKKGLATAKQRLGRILKIHRNG
KLLL

BDBM276077

n/a

Name

BDBM276077

Synonyms:

4-[2-[5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methylimidazol-4-yl]pyridin-4-yl]-1H-triazole-5-carbonitrile | US10071984, Example 39 | US10174003, Example 39

Type

Small organic molecule

Emp. Form.

C22H18FN7O

Mol. Mass.

415.423

SMILES

Cn1cnc(c1-c1ccc(F)cc1OCC1CC1)-c1cc(ccn1)-c1nn[nH]c1[N+]#[C-] |(2.9,-3.53,;1.41,-3.92,;.5,-5.17,;-.96,-4.69,;-.96,-3.15,;.5,-2.68,;.9,-1.19,;-.19,-.1,;.21,1.39,;1.7,1.78,;2.1,3.27,;2.79,.7,;2.39,-.79,;3.48,-1.88,;4.97,-1.48,;6.05,-2.57,;6.45,-4.06,;7.54,-2.97,;-2.3,-2.38,;-2.3,-.84,;-3.63,-.07,;-4.96,-.84,;-4.96,-2.38,;-3.63,-3.15,;-3.63,1.47,;-2.38,2.37,;-2.86,3.84,;-4.4,3.84,;-4.91,2.36,;-6.38,1.88,;-7.84,1.41,)|

Structure