Reaction Details Report a problem with these data
Target
Nuclear receptor ROR-gamma
Ligand
BDBM504165
Substrate
n/a
Meas. Tech.
Transcreener-Fluorecescence Polarization Assay
Ki
5.10±n/a nM
Citation
Bryan, MC; Do, S; Drobnick, J; Gobbi, A; Katsumoto, T; Kiefer, Jr., JR; Liang, J; Rajapaksa, NS; Chen, Y; Fu, L; Lai, KW; Liu, Z; Wai, J; Wang, F Pyrazolo[ 1,5a]pyrimidine derivatives as IRAK4 modulators US Patent US11034698 Publication Date 6/15/2021
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:
Human
Description:
P51449
Residue:
518
Sequence:
MDRAPQRQHRASRELLAAKKTHTSQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQRCNAAYSCTRQQNCPIDRTSRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLHAEVQKQLQQRQQQQQEPVVKTPPAGAQGADTLTYTLGLPDGQLPLGSSPDLPEASACPPGLLKASGSGPSYSNNLAKAGLNGASCHLEYSPERGKAEGRESFYSTGSQLTPDRCGLRFEEHRHPGLGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIFSREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEVVLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALYTALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHVERLQIFQHLHPIVVQAAFPPLYKELFSTETESPVGLSK
Inhibitor
Name:
BDBM504165
Synonyms:
N-(2,2-Dimethyl-6-(4-(2- (methylsulfonamido)ethyl)piper- azin-1-yl)-2,3- dihydrobenzofuran-5- yl)pyrazolo[1,5-a]pyrimidine-3- carboxamide | US11034698, Example 2
Type:
Small organic molecule
Emp. Form.:
C24H31N7O4S
Mol. Mass.:
513.612
SMILES:
CC1(C)Cc2cc(NC(=O)c3cnn4cccnc34)c(cc2O1)N1CCN(CCNS(C)(=O)=O)CC1