Target
Nuclear receptor ROR-gamma
Ligand
BDBM385415
Substrate
n/a
Meas. Tech.
Biological Assay for RORgammaT Activity
IC50
2.00±n/a nM
Citation
 Lapointe, BTFuller, PHGunaydin, HLiu, KScott, METrotter, BWZhang, H Substituted indazole compounds as RORgammaT inhibitors and uses thereof US Patent  US10689369 Publication Date 6/23/2020 
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:
BDBM385415
Synonyms:
4-((R or S)-1-(2-chloro- 6-cyclopropylbenzoyl)- 6-(5-oxa-2- azaspiro[3.4]octane-2- carbonyl)-4,5,6,7- tetrahydro-1H-indazol- 3-yl)cyclohex-3-ene-1- carboxylic acid | US10287272, Example 2X | US10689369, Example 2X
Type:
Small organic molecule
Emp. Form.:
C31H34ClN3O5
Mol. Mass.:
564.072
SMILES:
OC(=O)C1CCC(=CC1)c1nn(C(=O)c2c(Cl)cccc2C2CC2)c2CC(CCc12)C(=O)N1CC2(C1)CCCO2 |c:6|
Structure:
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