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Assay Detail

CHEMBL1039873

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of GS-red from human glucocorticoid receptor by fluorescent polarization assay
39
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.
Xiao HY, Wu DR, Malley MF, Gougoutas JZ, Habte SF, Cunningham MD, Somerville JE, Dodd JH, Barrish JC, Nadler SG, Dhar TG.
J Med Chem (2010) 53 : 1270 -1280
PubMed 20047280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 8.35 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310570 1 9.10
CHEMBL569044 1 9.00
CHEMBL569544 1 9.00
CHEMBL566600 1 9.00
CHEMBL384467 DEXAMETHASONE 4.0 1 8.92
CHEMBL572329 1 8.82
CHEMBL572356 1 8.74
CHEMBL572355 1 8.70
CHEMBL584258 1 8.70
CHEMBL577945 1 8.70
CHEMBL576472 1 8.70
CHEMBL567027 1 8.70
CHEMBL583625 1 8.70
CHEMBL567028 1 8.70
CHEMBL566823 1 8.70
CHEMBL572357 1 8.60
CHEMBL566575 1 8.60
CHEMBL311662 1 8.60
CHEMBL584522 1 8.59
CHEMBL569290 1 8.52
CHEMBL572212 1 8.51
CHEMBL583629 1 8.41
CHEMBL572330 1 8.40
CHEMBL565320 1 8.37
CHEMBL569061 1 8.28
CHEMBL569543 4 8.15
CHEMBL566387 1 8.10
CHEMBL566391 2 8.10
CHEMBL567237 1 8.05
CHEMBL569100 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310570 Ki = 0.8 nM 9.10
CHEMBL569544 Ki = 1.0 nM 9.00
CHEMBL569044 Ki = 1.0 nM 9.00
CHEMBL566600 Ki = 1.0 nM 9.00
CHEMBL384467 DEXAMETHASONE Ki = 1.2 nM 8.92
CHEMBL572329 Ki = 1.5 nM 8.82
CHEMBL572356 Ki = 1.8 nM 8.74
CHEMBL572355 Ki = 2.0 nM 8.70
CHEMBL567027 Ki = 2.0 nM 8.70
CHEMBL576472 Ki = 2.0 nM 8.70
CHEMBL577945 Ki = 2.0 nM 8.70
CHEMBL584258 Ki = 2.0 nM 8.70
CHEMBL567028 Ki = 2.0 nM 8.70
CHEMBL583625 Ki = 2.0 nM 8.70
CHEMBL566823 Ki = 2.0 nM 8.70
CHEMBL572357 Ki = 2.5 nM 8.60
CHEMBL311662 Ki = 2.5 nM 8.60
CHEMBL566575 Ki = 2.5 nM 8.60
CHEMBL584522 Ki = 2.6 nM 8.59
CHEMBL569290 Ki = 3.0 nM 8.52
CHEMBL572212 Ki = 3.1 nM 8.51
CHEMBL583629 Ki = 3.9 nM 8.41
CHEMBL572330 Ki = 4.0 nM 8.40
CHEMBL565320 Ki = 4.3 nM 8.37
CHEMBL569061 Ki = 5.2 nM 8.28
CHEMBL569543 Ki = 7.0 nM 8.15
CHEMBL566391 Ki = 8.0 nM 8.10
CHEMBL566387 Ki = 7.9 nM 8.10
CHEMBL567237 Ki = 9.0 nM 8.05
CHEMBL566391 Ki = 9.0 nM 8.05
CHEMBL569100 Ki = 11.0 nM 7.96
CHEMBL583858 Ki = 21.0 nM 7.68
CHEMBL583858 Ki = 25.0 nM 7.60
CHEMBL583859 Ki = 31.0 nM 7.51
CHEMBL566818 Ki = 33.0 nM 7.48
CHEMBL569543 Ki = 36.0 nM 7.44
CHEMBL568868 Ki = 47.0 nM 7.33
CHEMBL569543 Ki = 134.0 nM 6.87
CHEMBL569543 Ki > 1150.0 nM -