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Target
Nuclear receptor ROR-gamma
Ligand
BDBM50536811
Substrate
n/a
Meas. Tech.
ChEMBL_1934537 (CHEMBL4480189)
EC50
1900±n/a nM
Citation
 René, O; Fauber, BP; Barnard, A; Chapman, K; Deng, Y; Eidenschenk, C; Everett, C; Gobbi, A; Johnson, AR; La, H; Norman, M; Salmon, G; Summerhill, S; Wong, H Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties. Bioorg Med Chem Lett 26:4455-4461 (2016) [PubMed]  Article 
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:
BDBM50536811
Synonyms:
CHEMBL4562607
Type:
Small organic molecule
Emp. Form.:
C25H29FN4O3S
Mol. Mass.:
484.586
SMILES:
C[C@H]1CC[C@H](c2ccccc2C#N)S(=O)(=O)N1Cc1ccc(cc1F)N1CCN(CC1)C(C)=O |r|
Structure:
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