Reaction Details | |||
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Report a problem with these data | |||
Target | Apelin receptor | ||
Ligand | BDBM269571 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | [35S]GTPgammaS Binding Assay | ||
EC50 | 5.20±n/a nM | ||
Citation | Chen, N; Chen, X; Chen, Y; Cheng, AC; Connors, RV; Deignan, J; Dransfield, PJ; Du, X; Fu, Z; Heath, JA; Horne, DB; Houze, J; Kaller, MR; Khakoo, AY; Kopecky, DJ; Lai, S; Ma, Z; McGee, LR; Medina, JC; Mihalic, JT; Nishimura, N; Olson, SH; Pattaropong, V; Swaminath, G; Wang, X; Yang, K; Yeh, W; Debenedetto, MV; Farrell, RP; Hedley, SJ; Judd, TC; Kayser, 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: |
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BDBM269571 | |||
n/a | |||
Name | BDBM269571 | ||
Synonyms: | (2S,3R)-N-(4-(2,6-dimethoxyphenyl)-5-(2-methyl-4-pyridinyl)-4H-1,2,4-triazol-3-yl)-3-(5-methyl-2-pyrimidinyl)-2-butanesulfonamide | US10058550, Example 85.0 | US10221162, Example 85.0 | US9845310, Example 85.0 | ||
Type | Small organic molecule | ||
Emp. Form. | C25H29N7O4S | ||
Mol. Mass. | 523.607 | ||
SMILES | COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@@H](C)[C@H](C)c2ncc(C)cn2)nnc1-c1ccnc(C)c1 |r,wU:16.17,18.19,(-6.76,1.22,;-5.43,.45,;-4.09,1.22,;-4.09,2.76,;-2.76,3.53,;-1.42,2.76,;-1.42,1.22,;-.09,.45,;1.24,1.22,;-2.76,.45,;-2.76,-1.09,;-1.51,-1.99,;-.18,-1.22,;1.15,-1.99,;.38,-3.33,;1.92,-3.33,;2.49,-1.22,;2.49,.32,;3.82,-1.99,;3.82,-3.53,;5.16,-1.22,;6.49,-1.99,;7.82,-1.22,;7.82,.32,;9.16,1.09,;6.49,1.09,;5.16,.32,;-1.99,-3.46,;-3.53,-3.46,;-4,-1.99,;-5.49,-1.59,;-5.89,-.11,;-7.38,.29,;-8.47,-.8,;-8.07,-2.28,;-9.16,-3.37,;-6.58,-2.68,)| | ||
Structure |