Reaction Details |
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Target | Nuclear receptor ROR-gamma |
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Ligand | BDBM392006 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1989650 (CHEMBL4623385) |
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IC50 | 2.6±n/a nM |
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Citation | Steeneck, C; Gege, C; Kinzel, O; Albers, M; Kleymann, G; Schlüter, T; Schulz, A; Xue, X; Cummings, MD; Fourie, AM; Leonard, KA; Scott, B; Edwards, JP; Hoffmann, T; Goldberg, SD Discovery and optimization of new oxadiazole substituted thiazole ROR?t inverse agonists through a bioisosteric amide replacement approach. Bioorg Med Chem Lett30:0 (2020) [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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BDBM392006 |
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n/a |
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Name | BDBM392006 |
Synonyms: | US10301272, Example 6/4 |
Type | Small organic molecule |
Emp. Form. | C29H39N3O4S2 |
Mol. Mass. | 557.768 |
SMILES | CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(nc2CC2CCCCC2)C(=O)NCC(C)(C)O)c2ccccc12 |
Structure |
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