Reaction Details
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Target
Nuclear receptor ROR-gamma
Ligand
BDBM411409
Substrate
n/a
Meas. Tech.
TR-FRET (time-resolved fluorescence resonance energy transfer) assay
IC50
2.10±n/a nM
Citation
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More Info.:
Target
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:
MDRAPQRQHRASRELLAAKKTHTSQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQRCNAAYSCTRQQNCPIDRTSRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLHAEVQKQLQQRQQQQQEPVVKTPPAGAQGADTLTYTLGLPDGQLPLGSSPDLPEASACPPGLLKASGSGPSYSNNLAKAGLNGASCHLEYSPERGKAEGRESFYSTGSQLTPDRCGLRFEEHRHPGLGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIFSREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEVVLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALYTALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHVERLQIFQHLHPIVVQAAFPPLYKELFSTETESPVGLSK
Inhibitor
Name:
BDBM411409
Synonyms:
(R)-4-methyl-N-(1-methyl-3-(1-(2,3,3- trimethylbutanoyl)piperidin-4-yl)-1H-indol-5- yl)benzenesulfonamide | US10385036, Example 25
Type:
Small organic molecule
Emp. Form.:
C28H37N3O3S
Mol. Mass.:
495.677
SMILES:
C[C@@H](C(=O)N1CCC(CC1)c1cn(C)c2ccc(NS(=O)(=O)c3ccc(C)cc3)cc12)C(C)(C)C |r|