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Target
Relaxin receptor 1
Ligand
BDBM50449861
Substrate
n/a
Meas. Tech.
ChEMBL_1740775 (CHEMBL4156525)
EC50
47±n/a nM
Citation
 Wilson, KJ; Xiao, J; Chen, CZ; Huang, Z; Agoulnik, IU; Ferrer, M; Southall, N; Hu, X; Zheng, W; Xu, X; Wang, A; Myhr, C; Barnaeva, E; George, ER; Agoulnik, AI; Marugan, JJ Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile. Eur J Med Chem 156:79-92 (2018) [PubMed]  Article 
Target
Name:
Relaxin receptor 1
Synonyms:
LGR7 | Leucine-rich repeat-containing G-protein coupled receptor 7 | RXFP1 | RXFP1_HUMAN | Relaxin family peptide receptor 1
Type:
PROTEIN
Mol. Mass.:
86990.83
Organism:
Homo sapiens (Human)
Description:
ChEMBL_818426
Residue:
757
Sequence:
MTSGSVFFYILIFGKYFSHGGGQDVKCSLGYFPCGNITKCLPQLLHCNGVDDCGNQADEDNCGDNNGWSLQFDKYFASYYKMTSQYPFEAETPECLVGSVPVQCLCQGLELDCDETNLRAVPSVSSNVTAMSLQWNLIRKLPPDCFKNYHDLQKLYLQNNKITSISIYAFRGLNSLTKLYLSHNRITFLKPGVFEDLHRLEWLIIEDNHLSRISPPTFYGLNSLILLVLMNNVLTRLPDKPLCQHMPRLHWLDLEGNHIHNLRNLTFISCSNLTVLVMRKNKINHLNENTFAPLQKLDELDLGSNKIENLPPLIFKDLKELSQLNLSYNPIQKIQANQFDYLVKLKSLSLEGIEISNIQQRMFRPLMNLSHIYFKKFQYCGYAPHVRSCKPNTDGISSLENLLASIIQRVFVWVVSAVTCFGNIFVICMRPYIRSENKLYAMSIISLCCADCLMGIYLFVIGGFDLKFRGEYNKHAQLWMESTHCQLVGSLAILSTEVSVLLLTFLTLEKYICIVYPFRCVRPGKCRTITVLILIWITGFIVAFIPLSNKEFFKNYYGTNGVCFPLHSEDTESIGAQIYSVAIFLGINLAAFIIIVFSYGSMFYSVHQSAITATEIRNQVKKEMILAKRFFFIVFTDALCWIPIFVVKFLSLLQVEIPGTITSWVVIFILPINSALNPILYTLTTRPFKEMIHRFWYNYRQRKSMDSKGQKTYAPSFIWVEMWPLQEMPPELMKPDLFTYPCEMSLISQSTRLNSYS
  
Inhibitor
Name:
BDBM50449861
Synonyms:
CHEMBL3715081
Type:
Small organic molecule
Emp. Form.:
C25H23F3N2O5S
Mol. Mass.:
520.521
SMILES:
CCCCOc1ccccc1C(=O)Nc1ccccc1C(=O)Nc1cccc(c1)S(=O)(=O)C(F)(F)F
Structure:
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