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Reaction Details
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TargetApelin receptor
LigandBDBM269870
Substrate/Competitorn/a
Meas. Tech.[35S]GTPgammaS Binding Assay
EC50 0.900±n/a nM
Citation Chen, NChen, XChen, YCheng, ACConnors, RVDeignan, JDransfield, PJDu, XFu, ZHeath, JAHorne, DBHouze, JKaller, MRKhakoo, AYKopecky, DJLai, SMa, ZMcGee, LRMedina, JCMihalic, JTNishimura, NOlson, SHPattaropong, VSwaminath, GWang, XYang, KYeh, WDebenedetto, MVFarrell, RPHedley, SJJudd, TCKayser, F Triazole agonists of the APJ receptor US Patent US10221162 Publication Date 3/5/2019
More Info.:Get all data from this article,  Assay Method
 
Apelin receptor
Name:Apelin receptor
Synonyms:AGTRL1 | APJ | APJ_HUMAN | APLNR | Angiotensin receptor-like 1 | Apelin receptor | Apelin receptor (APJ) | G-protein coupled receptor APJ | G-protein coupled receptor HG11
Type:Enzyme Catalytic Domain
Mol. Mass.:42664.06
Organism:Homo sapiens (Human)
Description:P35414
Residue:380
Sequence:
MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREK
RRSADIFIASLAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCL
TGLSFDRYLAIVRPVANARLRLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQ
CYMDYSMVATVSSEWAWEVGLGVSSTTVGFVVPFTIMLTCYFFIAQTIAGHFRKERIEGL
RKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWPCDFDLFLMNIFPYCTCISYV
NSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGHSQGPGPNMGK
GGEQMHEKSIPYSQETLVVD
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BDBM269870
n/a
NameBDBM269870
Synonyms:(1S,2R)—N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-1-(2-methoxyethoxy)-1-(5-methylpyrimidin-2-yl)propane-2-sulfonamide or (1R,2S)—N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-1-(2-methoxyethoxy)-1-(5-methylpyrimidin-2-yl)propane-2-sulfonamide | US10058550, Example 396.0 | US10221162, Example 397.0 | US9845310, Example 397.0
TypeSmall organic molecule
Emp. Form.C27H33N7O6S
Mol. Mass.583.659
SMILESCOCCO[C@H]([C@@H](C)S(=O)(=O)Nc1nnc(-c2cncc(C)c2)n1-c1c(OC)cccc1OC)c1ncc(C)cn1 |r,wD:5.4,6.6,(6.64,-12.26,;6.64,-10.72,;5.31,-9.95,;5.31,-8.41,;3.98,-7.64,;3.98,-6.1,;2.64,-5.33,;2.64,-3.79,;1.31,-6.1,;.54,-7.43,;2.08,-7.43,;-.03,-5.33,;-1.36,-6.1,;-1.84,-7.57,;-3.38,-7.57,;-3.85,-6.1,;-5.34,-5.7,;-6.11,-7.04,;-7.65,-7.04,;-8.42,-5.7,;-7.65,-4.37,;-8.42,-3.04,;-6.11,-4.37,;-2.61,-5.2,;-2.61,-3.66,;-1.22,-2.91,;.11,-3.68,;1.44,-2.91,;-1.27,-1.35,;-2.61,-.58,;-3.94,-1.35,;-3.94,-2.89,;-5.27,-3.66,;-6.61,-2.89,;5.31,-5.33,;6.64,-6.1,;7.98,-5.33,;7.98,-3.79,;9.31,-3.02,;6.64,-3.02,;5.31,-3.79,)|
Structure
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