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Target
Nuclear receptor ROR-gamma
Ligand
BDBM20177
Substrate
n/a
Meas. Tech.
ChEMBL_1442780 (CHEMBL3375302)
EC50
20±n/a nM
Citation
van Niel, MB; Fauber, BP; Cartwright, M; Gaines, S; Killen, JC; René, O; Ward, SI; de Leon Boenig, G; Deng, Y; Eidenschenk, C; Everett, C; Gancia, E; Ganguli, A; Gobbi, A; Hawkins, J; Johnson, AR; Kiefer, JR; La, H; Lockey, P; Norman, M; Ouyang, W; Qin, A; Wakes, N; Waszkowycz, B; Wong, H A reversed sulfonamide series of selective RORc inverse agonists. Bioorg Med Chem Lett 24:5769-76 (2014) [PubMed] Article
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:
BDBM20177
Synonyms:
(1S,2R,5S,10S,11S,14R,15S)-14-[(2S,3R)-3-hydroxy-6-methylheptan-2-yl]-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-7-en-5-ol | 22(R)-hydroxycholesterol | CHEMBL422904
Type:
Steroid
Emp. Form.:
C27H46O2
Mol. Mass.:
402.6529
SMILES:
[H][C@@](O)(CCC(C)C)[C@@H](C)[C@@]1([H])CC[C@@]2([H])[C@]3([H])CC=C4C[C@@]([H])(O)CC[C@]4(C)[C@@]3([H])CC[C@]12C |r,t:19|