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Assay Detail

CHEMBL896645

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Functional
Agonist activity at GR by GRE activation assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.
Ardecky RJ, Hudson AR, Phillips DP, Tyhonas JS, Deckhut C, Lau TL, Li Y, Martinborough EA, Roach SL, Higuchi RI, Lopez FJ, Marschke KB, Miner JN, Karanewsky DS, Negro-Vilar A, Zhi L.
Bioorg Med Chem Lett (2007) 17 : 4158 -4162
PubMed 17553679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 7.89 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243455 1 9.70
CHEMBL3706960 1 9.70
CHEMBL3706932 1 9.22
CHEMBL3706962 1 9.15
CHEMBL3706956 1 8.96
CHEMBL3706946 1 8.82
CHEMBL3706961 1 8.82
CHEMBL3706934 1 8.47
CHEMBL3706935 1 8.35
CHEMBL3706936 1 8.29
CHEMBL131 PREDNISOLONE 4.0 1 8.28
CHEMBL3706938 1 8.26
CHEMBL3706940 1 7.80
CHEMBL3706933 1 7.75
CHEMBL3706955 1 7.48
CHEMBL3706952 1 7.42
CHEMBL3706951 1 7.37
CHEMBL3706937 1 7.10
CHEMBL3706939 1 6.97
CHEMBL3706957 1 6.88
CHEMBL3706942 1 6.72
CHEMBL3706953 1 6.68
CHEMBL3706941 1 6.45
CHEMBL3706958 1 6.36
CHEMBL3706954 1 6.34
CHEMBL3706950 1 -
CHEMBL3706949 1 -
CHEMBL3706948 1 -
CHEMBL3706947 1 -
CHEMBL3706945 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243455 EC50 = 0.2 nM 9.70
CHEMBL3706960 EC50 = 0.2 nM 9.70
CHEMBL3706932 EC50 = 0.6 nM 9.22
CHEMBL3706962 EC50 = 0.7 nM 9.15
CHEMBL3706956 EC50 = 1.1 nM 8.96
CHEMBL3706946 EC50 = 1.5 nM 8.82
CHEMBL3706961 EC50 = 1.5 nM 8.82
CHEMBL3706934 EC50 = 3.4 nM 8.47
CHEMBL3706935 EC50 = 4.5 nM 8.35
CHEMBL3706936 EC50 = 5.1 nM 8.29
CHEMBL131 PREDNISOLONE EC50 = 5.3 nM 8.28
CHEMBL3706938 EC50 = 5.5 nM 8.26
CHEMBL3706940 EC50 = 16.0 nM 7.80
CHEMBL3706933 EC50 = 18.0 nM 7.75
CHEMBL3706955 EC50 = 33.0 nM 7.48
CHEMBL3706952 EC50 = 38.0 nM 7.42
CHEMBL3706951 EC50 = 43.0 nM 7.37
CHEMBL3706937 EC50 = 79.0 nM 7.10
CHEMBL3706939 EC50 = 108.0 nM 6.97
CHEMBL3706957 EC50 = 133.0 nM 6.88
CHEMBL3706942 EC50 = 192.0 nM 6.72
CHEMBL3706953 EC50 = 207.0 nM 6.68
CHEMBL3706941 EC50 = 356.0 nM 6.45
CHEMBL3706958 EC50 = 437.0 nM 6.36
CHEMBL3706954 EC50 = 455.0 nM 6.34
CHEMBL3706950 EC50 > 1000.0 nM -
CHEMBL3706949 EC50 > 1000.0 nM -
CHEMBL3706948 EC50 > 1000.0 nM -
CHEMBL3706947 EC50 > 1000.0 nM -
CHEMBL3706945 EC50 > 1000.0 nM -
CHEMBL3706944 EC50 > 1000.0 nM -
CHEMBL3706943 EC50 > 1000.0 nM -