Reaction Details |
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Target | Relaxin receptor 1 |
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Ligand | BDBM50449859 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1740775 (CHEMBL4156525) |
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EC50 | 67±n/a nM |
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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 Chem156:79-92 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Relaxin receptor 1 |
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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: | MTSGSVFFYILIFGKYFSHGGGQDVKCSLGYFPCGNITKCLPQLLHCNGVDDCGNQADED
NCGDNNGWSLQFDKYFASYYKMTSQYPFEAETPECLVGSVPVQCLCQGLELDCDETNLRA
VPSVSSNVTAMSLQWNLIRKLPPDCFKNYHDLQKLYLQNNKITSISIYAFRGLNSLTKLY
LSHNRITFLKPGVFEDLHRLEWLIIEDNHLSRISPPTFYGLNSLILLVLMNNVLTRLPDK
PLCQHMPRLHWLDLEGNHIHNLRNLTFISCSNLTVLVMRKNKINHLNENTFAPLQKLDEL
DLGSNKIENLPPLIFKDLKELSQLNLSYNPIQKIQANQFDYLVKLKSLSLEGIEISNIQQ
RMFRPLMNLSHIYFKKFQYCGYAPHVRSCKPNTDGISSLENLLASIIQRVFVWVVSAVTC
FGNIFVICMRPYIRSENKLYAMSIISLCCADCLMGIYLFVIGGFDLKFRGEYNKHAQLWM
ESTHCQLVGSLAILSTEVSVLLLTFLTLEKYICIVYPFRCVRPGKCRTITVLILIWITGF
IVAFIPLSNKEFFKNYYGTNGVCFPLHSEDTESIGAQIYSVAIFLGINLAAFIIIVFSYG
SMFYSVHQSAITATEIRNQVKKEMILAKRFFFIVFTDALCWIPIFVVKFLSLLQVEIPGT
ITSWVVIFILPINSALNPILYTLTTRPFKEMIHRFWYNYRQRKSMDSKGQKTYAPSFIWV
EMWPLQEMPPELMKPDLFTYPCEMSLISQSTRLNSYS
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BDBM50449859 |
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n/a |
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Name | BDBM50449859 |
Synonyms: | CHEMBL3718400 |
Type | Small organic molecule |
Emp. Form. | C23H16F6N2O5S |
Mol. Mass. | 546.439 |
SMILES | FC(F)(F)COc1ccccc1C(=O)Nc1ccccc1C(=O)Nc1cccc(c1)S(=O)(=O)C(F)(F)F |
Structure |
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