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

CHEMBL2428212

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

Binding
Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization assay
ChEMBL ↗
47
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

Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.
Sheppeck JE, Gilmore JL, Xiao HY, Dhar TG, Nirschl D, Doweyko AM, Sack JS, Corbett MJ, Malley MF, Gougoutas JZ, Mckay L, Cunningham MD, Habte SF, Dodd JH, Nadler SG, Somerville JE, Barrish JC.
Bioorg Med Chem Lett (2013) 23 : 5442 -5447
PubMed 23953070 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 8.11 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2426624 — — 2 9.32
CHEMBL2426648 — — 1 9.05
CHEMBL1801004 — — 1 8.96
CHEMBL2426639 — — 1 8.96
CHEMBL384467 DEXAMETHASONE 4.0 1 8.92
CHEMBL2426636 — — 1 8.77
CHEMBL2426650 — — 1 8.72
CHEMBL2426623 — — 2 8.62
CHEMBL2426637 — — 1 8.62
CHEMBL2426658 — — 1 8.57
CHEMBL2426649 — — 1 8.40
CHEMBL2426660 — — 1 8.30
CHEMBL2426662 — — 1 8.29
CHEMBL2426656 — — 1 8.24
CHEMBL2426665 — — 1 8.22
CHEMBL2426663 — — 1 8.17
CHEMBL2426653 — — 1 8.14
CHEMBL2426638 — — 1 8.12
CHEMBL2426644 — — 1 8.10
CHEMBL2426647 — — 1 8.09
CHEMBL2426652 — — 1 8.06
CHEMBL2426635 — — 1 8.01
CHEMBL2426654 — — 1 8.00
CHEMBL2426625 — — 1 7.96
CHEMBL2426643 — — 1 7.96
CHEMBL2426627 — — 1 7.96
CHEMBL2426633 — — 1 7.92
CHEMBL2426642 — — 1 7.92
CHEMBL2426659 — — 1 7.89
CHEMBL2426631 — — 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2426624 — Ki = 0.48 nM 9.32
CHEMBL2426624 — Ki = 0.59 nM 9.23
CHEMBL2426648 — Ki = 0.9 nM 9.05
CHEMBL1801004 — Ki = 1.1 nM 8.96
CHEMBL2426639 — Ki = 1.1 nM 8.96
CHEMBL384467 DEXAMETHASONE Ki = 1.2 nM 8.92
CHEMBL2426636 — Ki = 1.7 nM 8.77
CHEMBL2426650 — Ki = 1.9 nM 8.72
CHEMBL2426623 — Ki = 2.4 nM 8.62
CHEMBL2426637 — Ki = 2.4 nM 8.62
CHEMBL2426658 — Ki = 2.7 nM 8.57
CHEMBL2426649 — Ki = 4.0 nM 8.40
CHEMBL2426660 — Ki = 5.0 nM 8.30
CHEMBL2426662 — Ki = 5.1 nM 8.29
CHEMBL2426656 — Ki = 5.7 nM 8.24
CHEMBL2426665 — Ki = 6.0 nM 8.22
CHEMBL2426663 — Ki = 6.7 nM 8.17
CHEMBL2426653 — Ki = 7.2 nM 8.14
CHEMBL2426638 — Ki = 7.5 nM 8.12
CHEMBL2426644 — Ki = 7.9 nM 8.10
CHEMBL2426647 — Ki = 8.1 nM 8.09
CHEMBL2426652 — Ki = 8.8 nM 8.06
CHEMBL2426635 — Ki = 9.8 nM 8.01
CHEMBL2426654 — Ki = 10.0 nM 8.00
CHEMBL2426625 — Ki = 11.0 nM 7.96
CHEMBL2426643 — Ki = 11.0 nM 7.96
CHEMBL2426627 — Ki = 11.0 nM 7.96
CHEMBL2426633 — Ki = 12.0 nM 7.92
CHEMBL2426642 — Ki = 12.0 nM 7.92
CHEMBL2426659 — Ki = 13.0 nM 7.89
CHEMBL2426631 — Ki = 14.0 nM 7.85
CHEMBL2426628 — Ki = 14.0 nM 7.85
CHEMBL2426664 — Ki = 15.0 nM 7.82
CHEMBL2426626 — Ki = 17.0 nM 7.77
CHEMBL2426630 — Ki = 17.0 nM 7.77
CHEMBL2426645 — Ki = 18.0 nM 7.75
CHEMBL2426641 — Ki = 18.0 nM 7.75
CHEMBL2426661 — Ki = 18.0 nM 7.75
CHEMBL2426655 — Ki = 19.0 nM 7.72
CHEMBL2426640 — Ki = 21.0 nM 7.68
CHEMBL2426629 — Ki = 21.0 nM 7.68
CHEMBL2426646 — Ki = 29.0 nM 7.54
CHEMBL2426651 — Ki = 36.0 nM 7.44
CHEMBL2426623 — Ki = 44.0 nM 7.36
CHEMBL2426632 — Ki = 46.0 nM 7.34
CHEMBL2426657 — Ki = 47.0 nM 7.33
CHEMBL2426634 — Ki = 84.0 nM 7.08