Reaction Details | |||
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Report a problem with these data | |||
Target | Apelin receptor | ||
Ligand | BDBM269710 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | [35S]GTPgammaS Binding Assay | ||
EC50 | 9.70±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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BDBM269710 | |||
n/a | |||
Name | BDBM269710 | ||
Synonyms: | (2S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-fluoro-3-pyridinyl)-4H-1,2,4-triazol-3-yl)-1-(5-fluoro-2-pyrimidinyl)-2-propanesulfonamide, (2R)-N-(4-(2,6-dimethoxyphenyl)-5-(5-fluoro-3-pyridinyl)-4H-1,2,4-triazol-3-yl)-1-(5-fluoro-2-pyrimidinyl)-2-propanesulfonamide | US10058550, Example 225.0 | US10058550, Example 226.0 | US10058550, Example 227.0 | US10221162, Example 227.0 | US9845310, Example 227.0 | ||
Type | Small organic molecule | ||
Emp. Form. | C22H21F2N7O4S | ||
Mol. Mass. | 517.508 | ||
SMILES | COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@@H](C)Cc2ncc(F)cn2)nnc1-c1cncc(F)c1 |r,wU:16.17,(-7.03,5.9,;-5.69,5.13,;-4.36,5.9,;-4.36,7.44,;-3.02,8.21,;-1.69,7.44,;-1.69,5.9,;-.36,5.13,;.98,5.9,;-3.02,5.13,;-3.02,3.59,;-1.78,2.68,;-.45,3.45,;.89,2.68,;.12,1.35,;1.66,1.35,;2.22,3.45,;2.22,4.99,;3.56,2.68,;4.89,3.45,;6.22,2.68,;7.56,3.45,;7.56,4.99,;8.89,5.76,;6.22,5.76,;4.89,4.99,;-2.25,1.22,;-3.79,1.22,;-4.27,2.68,;-5.81,2.68,;-6.58,1.35,;-8.12,1.35,;-8.89,2.68,;-8.12,4.02,;-8.89,5.35,;-6.58,4.02,)| | ||
Structure |