Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL833648

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

Functional
Inhibition of glucocorticoid receptor dependent alkaline phosphatase activity
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
von Geldern TW, Tu N, Kym PR, Link JT, Jae HS, Lai C, Apelqvist T, Rhonnstad P, Hagberg L, Koehler K, Grynfarb M, Goos-Nilsson A, Sandberg J, Osterlund M, Barkhem T, Höglund M, Wang J, Fung S, Wilcox D, Nguyen P, Jakob C, Hutchins C, Färnegårdh M, Kauppi B, Ohman L, Jacobson PB.
J Med Chem (2004) 47 : 4213 -4230
PubMed 15293993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.19 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406064 1 9.42
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.36
CHEMBL266673 1 9.12
CHEMBL427568 2 8.96
CHEMBL2096708 1 8.96
CHEMBL415621 1 8.96
CHEMBL408376 1 8.92
CHEMBL364368 1 8.85
CHEMBL266935 1 8.85
CHEMBL265125 1 8.57
CHEMBL409123 1 8.37
CHEMBL414318 1 8.07
CHEMBL2096804 1 7.92
CHEMBL406027 1 7.82
CHEMBL384975 1 7.82
CHEMBL407672 1 7.43
CHEMBL414041 1 7.43
CHEMBL263942 1 7.31
CHEMBL411185 1 7.30
CHEMBL440251 1 7.28
CHEMBL266656 1 7.00
CHEMBL436859 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406064 Ki = 0.38 nM 9.42
CHEMBL1276308 MIFEPRISTONE Ki = 0.44 nM 9.36
CHEMBL266673 Ki = 0.76 nM 9.12
CHEMBL427568 Ki = 1.1 nM 8.96
CHEMBL2096708 Ki = 1.1 nM 8.96
CHEMBL415621 Ki = 1.1 nM 8.96
CHEMBL408376 Ki = 1.2 nM 8.92
CHEMBL364368 Ki = 1.4 nM 8.85
CHEMBL266935 Ki = 1.4 nM 8.85
CHEMBL265125 Ki = 2.7 nM 8.57
CHEMBL409123 Ki = 4.3 nM 8.37
CHEMBL414318 Ki = 8.6 nM 8.07
CHEMBL427568 Ki = 11.0 nM 7.96
CHEMBL2096804 Ki = 12.0 nM 7.92
CHEMBL384975 Ki = 15.0 nM 7.82
CHEMBL406027 Ki = 15.0 nM 7.82
CHEMBL407672 Ki = 37.0 nM 7.43
CHEMBL414041 Ki = 37.0 nM 7.43
CHEMBL263942 Ki = 49.0 nM 7.31
CHEMBL411185 Ki = 50.0 nM 7.30
CHEMBL440251 Ki = 52.0 nM 7.28
CHEMBL266656 Ki = 100.0 nM 7.00
CHEMBL436859 Ki = 250.0 nM 6.60