Target
Nuclear receptor ROR-gamma
Ligand
BDBM50203493
Substrate
n/a
Meas. Tech.
ChEMBL_1625734 (CHEMBL3868203)
IC50
120±n/a nM
Citation
 Ouvry, GBouix-Peter, CCiesielski, FChantalat, LChristin, OComino, CDuvert, DFeret, CHarris, CSLamy, LLuzy, APMusicki, BOrfila, DPascau, JParnet, VPerrin, APierre, RPolge, GRaffin, CRival, YTaquet, NThoreau, EHennequin, LF Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists. Bioorg Med Chem Lett 26:5802-5808 (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:
BDBM50203493
Synonyms:
CHEMBL3912204
Type:
Small organic molecule
Emp. Form.:
C24H20ClN3O4
Mol. Mass.:
449.886
SMILES:
CN(C)C(=O)c1ccc2n(nc(Oc3c(C)cccc3Cl)c2c1)-c1ccc(cc1)C(O)=O
Structure:
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