Reaction Details Report a problem with these data
Target
Nuclear receptor ROR-alpha
Ligand
BDBM50452782
Substrate
n/a
Meas. Tech.
ChEMBL_1748338 (CHEMBL4182848)
EC50
>2000±n/a nM
Citation
Gong, H; Weinstein, DS; Lu, Z; Duan, JJ; Stachura, S; Haque, L; Karmakar, A; Hemagiri, H; Raut, DK; Gupta, AK; Khan, J; Camac, D; Sack, JS; Pudzianowski, A; Wu, DR; Yarde, M; Shen, DR; Borowski, V; Xie, JH; Sun, H; D'Arienzo, C; Dabros, M; Galella, MA; Wang, F; Weigelt, CA; Zhao, Q; Foster, W; Somerville, JE; Salter-Cid, LM; Barrish, JC; Carter, PH; Dhar, TGM Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (ROR?/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity. Bioorg Med Chem Lett 28:85-93 (2018) [PubMed] Article
More Info.:
Target
Name:
Nuclear receptor ROR-alpha
Synonyms:
NR1F1 | Nuclear receptor RZR-alpha | Nuclear receptor subfamily 1 group F member 1 | RAR-related orphan receptor A | RORA | RORA_HUMAN | RZRA | Retinoid-related orphan receptor-alpha
Type:
PROTEIN
Mol. Mass.:
58976.26
Organism:
Homo sapiens (Human)
Description:
ChEMBL_101591
Residue:
523
Sequence:
MESAPAAPDPAASEPGSSGADAAAGSRETPLNQESARKSEPPAPVRRQSYSSTSRGISVTKKTHTSQIEIIPCKICGDKSSGIHYGVITCEGCKGFFRRSQQSNATYSCPRQKNCLIDRTSRNRCQHCRLQKCLAVGMSRDAVKFGRMSKKQRDSLYAEVQKHRMQQQQRDHQQQPGEAEPLTPTYNISANGLTELHDDLSNYIDGHTPEGSKADSAVSSFYLDIQPSPDQSGLDINGIKPEPICDYTPASGFFPYCSFTNGETSPTVSMAELEHLAQNISKSHLETCQYLREELQQITWQTFLQEEIENYQNKQREVMWQLCAIKITEAIQYVVEFAKRIDGFMELCQNDQIVLLKAGSLEVVFIRMCRAFDSQNNTVYFDGKYASPDVFKSLGCEDFISFVFEFGKSLCSMHLTEDEIALFSAFVLMSADRSWLQEKVKIEKLQQKIQLALQHVLQKNHREDGILTKLICKVSTLRALCGRHTEKLMAFKAIYPDIVRLHFPPLYKELFTSEFEPAMQIDG