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Assay Detail

CHEMBL3266131

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Binding
Binding affinity to human glucocorticoid receptor by fluorescence polarization assay
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL2034) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.
Edman K, Ahlgren R, Bengtsson M, Bladh H, Bäckström S, Dahmén J, Henriksson K, Hillertz P, Hulikal V, Jerre A, Kinchin L, Kåse C, Lepistö M, Mile I, Nilsson S, Smailagic A, Taylor J, Tjörnebo A, Wissler L, Hansson T.
Bioorg Med Chem Lett (2014) 24 : 2571 -2577
PubMed 24755427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 7.57 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3261408 — — 1 8.64
CHEMBL3261425 — — 1 8.52
CHEMBL3261413 — — 1 8.47
CHEMBL3261410 — — 1 8.46
CHEMBL3261409 — — 1 8.42
CHEMBL3261423 — — 1 8.42
CHEMBL3261424 — — 1 8.42
CHEMBL3261415 — — 1 8.41
CHEMBL3261417 — — 1 8.40
CHEMBL3261414 — — 1 8.39
CHEMBL3261420 — — 1 8.34
CHEMBL3261427 — — 1 8.33
CHEMBL3261407 — — 1 8.31
CHEMBL3261406 — — 1 8.28
CHEMBL3261411 — — 1 8.28
CHEMBL3261419 — — 1 8.27
CHEMBL3261412 — — 1 8.25
CHEMBL3261428 — — 1 8.24
CHEMBL3261418 — — 1 8.16
CHEMBL3261421 — — 1 8.11
CHEMBL3261426 — — 1 7.92
CHEMBL3261174 — — 1 7.75
CHEMBL3261167 — — 1 7.75
CHEMBL3261169 — — 1 7.64
CHEMBL3261429 — — 1 7.64
CHEMBL3261404 — — 1 7.50
CHEMBL3261416 — — 1 7.46
CHEMBL3261170 — — 1 7.38
CHEMBL3261165 — — 1 7.26
CHEMBL3261171 — — 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3261408 — IC50 = 2.3 nM 8.64
CHEMBL3261425 — IC50 = 3.0 nM 8.52
CHEMBL3261413 — IC50 = 3.4 nM 8.47
CHEMBL3261410 — IC50 = 3.5 nM 8.46
CHEMBL3261409 — IC50 = 3.8 nM 8.42
CHEMBL3261423 — IC50 = 3.8 nM 8.42
CHEMBL3261424 — IC50 = 3.8 nM 8.42
CHEMBL3261415 — IC50 = 3.9 nM 8.41
CHEMBL3261417 — IC50 = 4.0 nM 8.40
CHEMBL3261414 — IC50 = 4.1 nM 8.39
CHEMBL3261420 — IC50 = 4.6 nM 8.34
CHEMBL3261427 — IC50 = 4.7 nM 8.33
CHEMBL3261407 — IC50 = 4.9 nM 8.31
CHEMBL3261406 — IC50 = 5.2 nM 8.28
CHEMBL3261411 — IC50 = 5.3 nM 8.28
CHEMBL3261419 — IC50 = 5.4 nM 8.27
CHEMBL3261412 — IC50 = 5.6 nM 8.25
CHEMBL3261428 — IC50 = 5.7 nM 8.24
CHEMBL3261418 — IC50 = 6.9 nM 8.16
CHEMBL3261421 — IC50 = 7.7 nM 8.11
CHEMBL3261426 — IC50 = 12.0 nM 7.92
CHEMBL3261167 — IC50 = 18.0 nM 7.75
CHEMBL3261174 — IC50 = 18.0 nM 7.75
CHEMBL3261169 — IC50 = 23.0 nM 7.64
CHEMBL3261429 — IC50 = 23.0 nM 7.64
CHEMBL3261404 — IC50 = 32.0 nM 7.50
CHEMBL3261416 — IC50 = 35.0 nM 7.46
CHEMBL3261170 — IC50 = 42.0 nM 7.38
CHEMBL3261165 — IC50 = 55.0 nM 7.26
CHEMBL3261171 — IC50 = 75.0 nM 7.12
CHEMBL3261177 — IC50 = 80.0 nM 7.10
CHEMBL3261166 — IC50 = 85.0 nM 7.07
CHEMBL3261405 — IC50 = 97.0 nM 7.01
CHEMBL3261175 — IC50 = 160.0 nM 6.80
CHEMBL3261398 — IC50 = 220.0 nM 6.66
CHEMBL3261168 — IC50 = 240.0 nM 6.62
CHEMBL3261403 — IC50 = 410.0 nM 6.39
CHEMBL3261422 — IC50 = 795.0 nM 6.10
CHEMBL3261176 — IC50 = 1600.0 nM 5.80
CHEMBL3261400 — IC50 = 1800.0 nM 5.75
CHEMBL3261172 — IC50 = 10000.0 nM 5.00
CHEMBL3261173 — IC50 = 10000.0 nM 5.00
CHEMBL3261399 — IC50 > 10000.0 nM -
CHEMBL3261401 — IC50 > 10000.0 nM -
CHEMBL3261402 — IC50 > 10000.0 nM -