Reaction Details | |||
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Report a problem with these data | |||
Target | Apelin receptor | ||
Ligand | BDBM269631 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | [35S]GTPγS Binding | ||
EC50 | 12.0±n/a nM | ||
Citation | Chen, N; Chen, X; Cheng, AC; Connors, RV; Deignan, J; Dransfield, PJ; Du, X; Fu, Z; Heath, JA; Horne, DB; Houze, J; Kaller, MR; Kopecky, DJ; Lai, S; Ma, Z; McGee, LR; Medina, JC; Mihalic, JT; Nishimura, N; Olson, SH; Pattaropong, V; Wang, X; Yang, K; Debenedetto, MV; Hedley, SJ Intermediates for preparing triazole agonists of the APJ receptor US Patent US9845310 Publication Date 12/19/2017 | ||
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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BDBM269631 | |||
n/a | |||
Name | BDBM269631 | ||
Synonyms: | (2S)-N-(4-(2,6-dimethoxyphenyl)-5-(4-methoxy-2-pyridinyl)-4H-1,2,4-triazol-3-yl)-1-(5-fluoro-2-pyrimidinyl)-2-propanesulfonamide, (2R)-N-(4-(2,6-dimethoxyphenyl)-5-(4-methoxy-2-pyridinyl)-4H-1,2,4-triazol-3-yl)-1-(5-fluoro-2-pyrimidinyl)-2-propanesulfonamide | US10058550, Example 145.0 | US10221162, Example 145.0 | US9845310, Example 145.0 | ||
Type | Small organic molecule | ||
Emp. Form. | C23H24FN7O5S | ||
Mol. Mass. | 529.544 | ||
SMILES | COc1ccnc(c1)-c1nnc(NS(=O)(=O)[C@@H](C)Cc2ncc(F)cn2)n1-c1c(OC)cccc1OC |r,wU:16.17,(-10.43,2.57,;-8.89,2.57,;-8.12,1.24,;-8.89,-.1,;-8.12,-1.43,;-6.58,-1.43,;-5.81,-.1,;-6.58,1.24,;-4.27,-.1,;-3.79,-1.56,;-2.25,-1.56,;-1.78,-.1,;-.45,.67,;.89,-.1,;.12,-1.43,;1.66,-1.43,;2.22,.67,;2.22,2.21,;3.56,-.1,;4.89,.67,;6.22,-.1,;7.56,.67,;7.56,2.21,;8.89,2.98,;6.22,2.98,;4.89,2.21,;-3.02,.81,;-3.02,2.35,;-1.69,3.12,;-.36,2.35,;.98,3.12,;-1.69,4.66,;-3.02,5.43,;-4.36,4.66,;-4.36,3.12,;-5.69,2.35,;-7.03,3.12,)| | ||
Structure |