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TargetLeucine-rich repeat serine/threonine-protein kinase 2 [970-2527,G2019S]
LigandBDBM223569
Substrate/Competitorn/a
Meas. Tech.Kinase Activity Assay
pH8.5±n/a
Temperature303.15±n/a K
IC50 760±n/a nM
Commentsextracted
Citation Mikkelsen, GKDavid, LWatson, SSmith, GPWilliamson, DSChen, I Aminopyridine derived compounds as LRRK2 inhibitors US Patent US9321748 Publication Date 4/26/2016
More Info.:Get all data from this article,  Assay Method
 
Leucine-rich repeat serine/threonine-protein kinase 2 [970-2527,G2019S]
Name:Leucine-rich repeat serine/threonine-protein kinase 2 [970-2527,G2019S]
Synonyms:LRRK2 | LRRK2_HUMAN | Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) (G2019S) | Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2)(G2019S) | PARK8
Type:Protein
Mol. Mass.:177347.59
Organism:Homo sapiens (Human)
Description:Human LRRK2 variant (970-2527aa) with G2019S mutation
Residue:1558
Sequence:
HSDSISSLASEREYITSLDLSANELRDIDALSQKCCISVHLEHLEKLELHQNALTSFPQQ
LCETLKSLTHLDLHSNKFTSFPSYLLKMSCIANLDVSRNDIGPSVVLDPTVKCPTLKQFN
LSYNQLSFVPENLTDVVEKLEQLILEGNKISGICSPLRLKELKILNLSKNHISSLSENFL
EACPKVESFSARMNFLAAMPFLPPSMTILKLSQNKFSCIPEAILNLPHLRSLDMSSNDIQ
YLPGPAHWKSLNLRELLFSHNQISILDLSEKAYLWSRVEKLHLSHNKLKEIPPEIGCLEN
LTSLDVSYNLELRSFPNEMGKLSKIWDLPLDELHLNFDFKHIGCKAKDIIRFLQQRLKKA
VPYNRMKLMIVGNTGSGKTTLLQQLMKTKKSDLGMQSATVGIDVKDWPIQIRDKRKRDLV
LNVWDFAGREEFYSTHPHFMTQRALYLAVYDLSKGQAEVDAMKPWLFNIKARASSSPVIL
VGTHLDVSDEKQRKACMSKITKELLNKRGFPAIRDYHFVNATEESDALAKLRKTIINESL
NFKIRDQLVVGQLIPDCYVELEKIILSERKNVPIEFPVIDRKRLLQLVRENQLQLDENEL
PHAVHFLNESGVLLHFQDPALQLSDLYFVEPKWLCKIMAQILTVKVEGCPKHPKGIISRR
DVEKFLSKKRKFPKNYMSQYFKLLEKFQIALPIGEEYLLVPSSLSDHRPVIELPHCENSE
IIIRLYEMPYFPMGFWSRLINRLLEISPYMLSGRERALRPNRMYWRQGIYLNWSPEAYCL
VGSEVLDNHPESFLKITVPSCRKGCILLGQVVDHIDSLMEEWFPGLLEIDICGEGETLLK
KWALYSFNDGEEHQKILLDDLMKKAEEGDLLVNPDQPRLTIPISQIAPDLILADLPRNIM
LNNDELEFEQAPEFLLGDGSFGSVYRAAYEGEEVAVKIFNKHTSLRLLRQELVVLCHLHH
PSLISLLAAGIRPRMLVMELASKGSLDRLLQQDKASLTRTLQHRIALHVADGLRYLHSAM
IIYRDLKPHNVLLFTLYPNAAIIAKIADYSIAQYCCRMGIKTSEGTPGFRAPEVARGNVI
YNQQADVYSFGLLLYDILTTGGRIVEGLKFPNEFDELEIQGKLPDPVKEYGCAPWPMVEK
LIKQCLKENPQERPTSAQVFDILNSAELVCLTRRILLPKNVIVECMVATHHNSRNASIWL
GCGHTDRGQLSFLDLNTEGYTSEEVADSRILCLALVHLPVEKESWIVSGTQSGTLLVINT
EDGKKRHTLEKMTDSVTCLYCNSFSKQSKQKNFLLVGTADGKLAIFEDKTVKLKGAAPLK
ILNIGNVSTPLMCLSESTNSTERNVMWGGCGTKIFSFSNDFTIQKLIETRTSQLFSYAAF
SDSNIITVVVDTALYIAKQNSPVVEVWDKKTEKLCGLIDCVHFLREVMVKENKESKHKMS
YSGRVKTLCLQKNTALWIGTGGGHILLLDLSTRRLIRVIYNFCNSVRVMMTAQLGSLKNV
MLVLGYNRKNTEGTQKQKEIQSCLTVWDINLPHEVQNLEKHIEVRKELAEKMRRTSVE
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  Blast E-value cutoff:
BDBM223569
n/a
NameBDBM223569
Synonyms:US9321748, 29
TypeSmall organic molecule
Emp. Form.C21H23N5O2
Mol. Mass.377.4396
SMILESNc1ncc(cc1-c1nnc(o1)C1CC1)-c1cccc(CN2CCOCC2)c1
Structure
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