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Target
Nuclear receptor ROR-gamma
Ligand
BDBM493606
Substrate
n/a
Meas. Tech.
ChEMBL_2123850 (CHEMBL4833083)
IC50
30±n/a nM
Citation
 Narjes, F; Llinas, A; von Berg, S; Jirholt, J; Lever, S; Pehrson, R; Collins, M; Malmberg, A; Svanberg, P; Xue, Y; Olsson, RI; Malmberg, J; Hughes, G; Hossain, N; Grindebacke, H; Leffler, A; Krutrök, N; Bäck, E; Ramnegård, M; Lepistö, M; Thunberg, L; Aagaard, A; McPheat, J; Hansson, EL; Chen, R; Xiong, Y; Hansson, TG AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2. J Med Chem 64:13807-13829 (2021) [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:
BDBM493606
Synonyms:
US10988445, Example 202
Type:
Small organic molecule
Emp. Form.:
C23H20F6N2O5S
Mol. Mass.:
550.471
SMILES:
OC(c1ccc(NC(=O)C2N(Cc3cc(ccc23)S(=O)(=O)CC2CC2)C=O)cc1)(C(F)(F)F)C(F)(F)F
Structure:
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