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TargetP2X purinoceptor 2/3
LigandBDBM319939
Substrate/Competitorn/a
Meas. Tech.Intracellular Calcium Measurement to Assess Antagonist Activity
IC50 41.0±n/a nM
Citation Davenport, AJBräuer, NFischer, OMRotgeri, ARottmann, ANeagoe, INagel, JGodinho-Coelho, AKlar, J 1,3-thiazol-2-yl substituted benzamides US Patent US10202369 Publication Date 2/12/2019
More Info.:Get all data from this article,  Assay Method
 
P2X purinoceptor 2/3
Name:P2X purinoceptor 2/3
Synonyms:P2X2/3 | P2X2/P2X3 heterotrimeric receptor
Type:Protein
Mol. Mass.:n/a
Description:n/a
Components:This complex has 2 components.
Component 1
Name:P2X purinoceptor 2
Synonyms:ATP receptor | P2RX2 | P2RX2_HUMAN | P2X2 | Purinergic receptor | PurinergicP2X2/3
Type:Enzyme Catalytic Domain
Mol. Mass.:51765.18
Organism:Homo sapiens (Human)
Description:PurinergicP2X2/3 0 HUMAN::Q9UBL9
Residue:471
Sequence:
MAAAQPKYPAGATARRLARGCWSALWDYETPKVIVVRNRRLGVLYRAVQLLILLYFVWYV
FIVQKSYQESETGPESSIITKVKGITTSEHKVWDVEEYVKPPEGGSVFSIITRVEATHSQ
TQGTCPESIRVHNATCLSDADCVAGELDMLGNGLRTGRCVPYYQGPSKTCEVFGWCPVED
GASVSQFLGTMAPNFTILIKNSIHYPKFHFSKGNIADRTDGYLKRCTFHEASDLYCPIFK
LGFIVEKAGESFTELAHKGGVIGVIINWDCDLDLPASECNPKYSFRRLDPKHVPASSGYN
FRFAKYYKINGTTTRTLIKAYGIRIDVIVHGQAGKFSLIPTIINLATALTSVGVGSFLCD
WILLTFMNKNKVYSHKKFDKVCTPSHPSGSWPVTLARVLGQAPPEPGHRSEDQHPSPPSG
QEGQQGAECGPAFPPLRPCPISAPSEQMVDTPASEPAQASTPTDPKGLAQL
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Component 2
Name:P2X purinoceptor 3
Synonyms:ATP receptor | Glucocorticoid receptor | P2RX3 | P2RX3_HUMAN | P2X purinoceptor 3 | P2X purinoceptor 3 (P2RX3) | P2X purinoceptor 3 (P2X3) | P2X3 | P2X3 purinoceptor | Purinergic receptor | p2x3 + hsa
Type:Protein
Mol. Mass.:44292.02
Organism:Homo sapiens (Human)
Description:P56373
Residue:397
Sequence:
MNCISDFFTYETTKSVVVKSWTIGIINRVVQLLIISYFVGWVFLHEKAYQVRDTAIESSV
VTKVKGSGLYANRVMDVSDYVTPPQGTSVFVIITKMIVTENQMQGFCPESEEKYRCVSDS
QCGPERLPGGGILTGRCVNYSSVLRTCEIQGWCPTEVDTVETPIMMEAENFTIFIKNSIR
FPLFNFEKGNLLPNLTARDMKTCRFHPDKDPFCPILRVGDVVKFAGQDFAKLARTGGVLG
IKIGWVCDLDKAWDQCIPKYSFTRLDSVSEKSSVSPGYNFRFAKYYKMENGSEYRTLLKA
FGIRFDVLVYGNAGKFNIIPTIISSVAAFTSVGVGTVLCDIILLNFLKGADQYKAKKFEE
VNETTLKIAALTNPVYPSDQTTAEKQSTDSGAFSIGH
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BDBM319939
n/a
NameBDBM319939
Synonyms:3-[(2-methylpyridin-4-yl)oxy]-N-[(1R)-1-(2-methylpyrimidin-5-yl)ethyl]-5-(5-methyl-1,3-thiazol-2-yl)benzamide | US10174016, Example 106 | US10202369, Example 106 | US10472354, Example 106
TypeSmall organic molecule
Emp. Form.C24H23N5O2S
Mol. Mass.445.537
SMILESC[C@@H](NC(=O)c1cc(Oc2ccnc(C)c2)cc(c1)-c1ncc(C)s1)c1cnc(C)nc1 |r|
Structure
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