Reaction Details |
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Target | Nuclear receptor ROR-gamma |
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Ligand | BDBM50541922 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2060118 (CHEMBL4715119) |
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EC50 | 12±n/a nM |
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Citation | Liu, Q; Xiao, HY; Batt, DG; Xiao, Z; Zhu, Y; Yang, MG; Li, N; Yip, S; Li, P; Sun, D; Wu, DR; Ruzanov, M; Sack, JS; Weigelt, CA; Wang, J; Li, S; Shuster, DJ; Xie, JH; Song, Y; Sherry, T; Obermeier, MT; Fura, A; Stefanski, K; Cornelius, G; Chacko, S; Khandelwal, P; Dudhgaonkar, S; Rudra, A; Nagar, J; Murali, V; Govindarajan, A; Denton, R; Zhao, Q; Meanwell, NA; Borzilleri, R; Dhar, TGM Azatricyclic Inverse Agonists of ROR?t That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis. ACS Med Chem Lett12:827-835 (2021) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Nuclear receptor ROR-gamma |
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Name: | Nuclear receptor ROR-gamma |
Synonyms: | NR1F3 | Nuclear receptor ROR-gamma | Nuclear receptor ROR-gamma (RORC) | Nuclear receptor subfamily 1 group F member 3 | RAR-related orphan receptor C (RORc) | RORC | RORG | RORG_HUMAN | RZRG | Retinoid-related orphan receptor-gamma | Retinoid-related orphan receptor-gamma (RORc) |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 58218.40 |
Organism: | Homo sapiens (Human) |
Description: | P51449 |
Residue: | 518 |
Sequence: | MDRAPQRQHRASRELLAAKKTHTSQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQR
CNAAYSCTRQQNCPIDRTSRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLHAEVQK
QLQQRQQQQQEPVVKTPPAGAQGADTLTYTLGLPDGQLPLGSSPDLPEASACPPGLLKAS
GSGPSYSNNLAKAGLNGASCHLEYSPERGKAEGRESFYSTGSQLTPDRCGLRFEEHRHPG
LGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIF
SREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEV
VLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALY
TALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHV
ERLQIFQHLHPIVVQAAFPPLYKELFSTETESPVGLSK
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BDBM50541922 |
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n/a |
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Name | BDBM50541922 |
Synonyms: | Bms-986251 |
Type | Small organic molecule |
Emp. Form. | C30H29F8NO5S |
Mol. Mass. | 667.607 |
SMILES | [H][C@@]12CCc3cc(ccc3[C@@]1(CCN2C(=O)[C@@H]1CC[C@H](C[C@@H]1C)C(O)=O)S(=O)(=O)c1ccc(F)cc1)C(F)(C(F)(F)F)C(F)(F)F |r| |
Structure |
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