Reaction Details |
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Target | Nuclear receptor ROR-gamma |
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Ligand | BDBM385477 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Biological Assay for RORgammaT Activity |
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IC50 | 1.000±n/a nM |
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Citation | Lapointe, BT; Fuller, PH; Gunaydin, H; Liu, K; Scott, ME; Trotter, BW; Zhang, H Substituted indazole compounds as RORgammaT inhibitors and uses thereof US Patent US10689369 Publication Date 6/23/2020 |
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More Info.: | Get all data from this article, Assay Method |
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Nuclear receptor ROR-gamma |
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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: | MDRAPQRQHRASRELLAAKKTHTSQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQR
CNAAYSCTRQQNCPIDRTSRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLHAEVQK
QLQQRQQQQQEPVVKTPPAGAQGADTLTYTLGLPDGQLPLGSSPDLPEASACPPGLLKAS
GSGPSYSNNLAKAGLNGASCHLEYSPERGKAEGRESFYSTGSQLTPDRCGLRFEEHRHPG
LGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIF
SREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEV
VLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALY
TALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHV
ERLQIFQHLHPIVVQAAFPPLYKELFSTETESPVGLSK
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BDBM385477 |
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n/a |
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Name | BDBM385477 |
Synonyms: | (R or S)-4-((R or 5)-1- (2-chloro-6-(1- (trifluoromethyl) cyclopropyl)benzoyl)-6- ((3S,4S)-3- (dimethylamino)-4- hydroxypyrrolidine-1- carbonyl)-4,5,6,7- tetrahydro-1H-indazol- 3-yl)cyclohex-3-ene-1- carboxylic acid | US10287272, Example 5V | US10689369, Example 5V |
Type | Small organic molecule |
Emp. Form. | C32H36ClF3N4O5 |
Mol. Mass. | 649.1 |
SMILES | CN(C)[C@H]1CN(C[C@@H]1O)C(=O)C1CCc2c(C1)n(nc2C1=CCC(CC1)C(O)=O)C(=O)c1c(Cl)cccc1C1(CC1)C(F)(F)F |r,t:23| |
Structure |
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