Ki Summary

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Target

Isoform 2 of Histone lysine demethylase PHF8 (2)

Ligand

BDBM276079

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

BDBM276079

n/a

Name

BDBM276079

Synonyms:

2-[5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methylimidazol-4-yl]-4-(5-fluoro-1H-triazol-4-yl)pyridine | US10071984, Example 41 | US10174003, Example 41 | US9896436, Example 41

Type

Small organic molecule

Emp. Form.

C21H18F2N6O

Mol. Mass.

408.404

SMILES

Cn1cnc(c1-c1ccc(F)cc1OCC1CC1)-c1cc(ccn1)-c1nn[nH]c1F |(2.23,-3.53,;.74,-3.92,;-.16,-5.17,;-1.63,-4.69,;-1.63,-3.15,;-.16,-2.68,;.23,-1.19,;-.85,-.1,;-.46,1.39,;1.03,1.78,;1.43,3.27,;2.12,.7,;1.72,-.79,;2.81,-1.88,;4.3,-1.48,;5.39,-2.57,;5.79,-4.06,;6.88,-2.97,;-2.96,-2.38,;-2.96,-.84,;-4.3,-.07,;-5.63,-.84,;-5.63,-2.38,;-4.3,-3.15,;-4.3,1.47,;-3.05,2.37,;-3.53,3.84,;-5.07,3.84,;-5.54,2.37,;-6.88,1.6,)|

Structure