BDBM220233 US9290476, 77A::US9290476, 77B::US9290476, 77C

SMILES COc1nc2ccc(cc2c(Cl)c1Cc1ccc(cc1)C(F)(F)F)C(O)(c1cnnn1C)c1ccc(C)nc1C

InChI Key InChIKey=HVSWHSCHDKSPHW-UHFFFAOYSA-N

Data  2 IC50  4 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 220233   

TargetNuclear receptor ROR-gamma(Human)
Janssen Research and Development

Curated by ChEMBL
LigandPNGBDBM220233(US9290476, 77C | US9290476, 77B | US9290476, 77A)
Affinity DataKd:  0.100nMAssay Description:Displacement of thermofluor from human recombinant N-terminal TEV cleavage site-fused-His-tagged RORgammat LBD expressed in Escherichia coli assessed...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetIsoform 2 of Nuclear receptor ROR-gamma (RORgT)(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM220233(US9290476, 77C | US9290476, 77B | US9290476, 77A)
Affinity DataKd:  0.140nMpH: 7.0 T: 2°CAssay Description:Bar-coded assay plates are robotically loaded onto a thermostatically controlled PCR-type thermal block and then heated at a typical ramp-rate of 1 &...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2017
Entry Details
US Patent

TargetIsoform 2 of Nuclear receptor ROR-gamma (RORgT)(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM220233(US9290476, 77C | US9290476, 77B | US9290476, 77A)
Affinity DataKd:  1.10nMpH: 7.0 T: 2°CAssay Description:Bar-coded assay plates are robotically loaded onto a thermostatically controlled PCR-type thermal block and then heated at a typical ramp-rate of 1 &...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2017
Entry Details
US Patent

TargetNuclear receptor ROR-gamma(Human)
Janssen Research and Development

Curated by ChEMBL
LigandPNGBDBM220233(US9290476, 77C | US9290476, 77B | US9290476, 77A)
Affinity DataIC50: 3.30nMAssay Description:Inverse agonist activity at RORgammat in human PBMC derived CD4-positive T cells assessed as suppression of T cell differentiation to Th17 cells by m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetNuclear receptor ROR-gamma(Human)
Janssen Research and Development

Curated by ChEMBL
LigandPNGBDBM220233(US9290476, 77C | US9290476, 77B | US9290476, 77A)
Affinity DataIC50: 3.90nMAssay Description:Inverse agonist activity at GAL4-DNA binding domain-fused human RORgammat LBD expressed in pGL4.31 transfected HEK293T cells assessed as inhibition o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
TargetIsoform 2 of Nuclear receptor ROR-gamma (RORgT)(Human)
Janssen Pharmaceutica

US Patent
LigandPNGBDBM220233(US9290476, 77C | US9290476, 77B | US9290476, 77A)
Affinity DataKd:  320nMpH: 7.0 T: 2°CAssay Description:Bar-coded assay plates are robotically loaded onto a thermostatically controlled PCR-type thermal block and then heated at a typical ramp-rate of 1 &...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2017
Entry Details
US Patent