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Assay Detail

CHEMBL932361

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

Binding
Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Aster SD, Graham DW, Kharbanda D, Patel G, Ponpipom M, Santorelli GM, Szymonifka MJ, Mundt SS, Shah K, Springer MS, Thieringer R, Hermanowski-Vosatka A, Wright SD, Xiao J, Zokian H, Balkovec JM.
Bioorg Med Chem Lett (2008) 18 : 2799 -2804
PubMed 18434143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 7.90 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL403898 1 9.01
CHEMBL258388 1 9.01
CHEMBL257779 1 9.01
CHEMBL256298 1 9.00
CHEMBL401909 1 8.89
CHEMBL403811 1 8.89
CHEMBL257601 1 8.85
CHEMBL401883 1 8.72
CHEMBL401908 1 8.70
CHEMBL401884 1 8.64
CHEMBL256986 1 8.59
CHEMBL401975 1 8.57
CHEMBL258389 1 8.54
CHEMBL257129 1 8.54
CHEMBL256158 1 8.51
CHEMBL402737 1 8.44
CHEMBL257963 1 8.41
CHEMBL257752 1 8.37
CHEMBL401830 1 8.34
CHEMBL401988 1 8.28
CHEMBL404638 1 8.24
CHEMBL428951 1 8.11
CHEMBL403758 1 8.05
CHEMBL257985 1 7.92
CHEMBL258165 1 7.89
CHEMBL403944 1 7.82
CHEMBL257364 1 7.70
CHEMBL404564 1 7.68
CHEMBL403369 1 7.58
CHEMBL253953 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL403898 IC50 = 0.98 nM 9.01
CHEMBL257779 IC50 = 0.98 nM 9.01
CHEMBL258388 IC50 = 0.98 nM 9.01
CHEMBL256298 IC50 = 1.0 nM 9.00
CHEMBL401909 IC50 = 1.3 nM 8.89
CHEMBL403811 IC50 = 1.3 nM 8.89
CHEMBL257601 IC50 = 1.4 nM 8.85
CHEMBL401883 IC50 = 1.9 nM 8.72
CHEMBL401908 IC50 = 2.0 nM 8.70
CHEMBL401884 IC50 = 2.3 nM 8.64
CHEMBL256986 IC50 = 2.6 nM 8.59
CHEMBL401975 IC50 = 2.7 nM 8.57
CHEMBL258389 IC50 = 2.9 nM 8.54
CHEMBL257129 IC50 = 2.9 nM 8.54
CHEMBL256158 IC50 = 3.1 nM 8.51
CHEMBL402737 IC50 = 3.6 nM 8.44
CHEMBL257963 IC50 = 3.9 nM 8.41
CHEMBL257752 IC50 = 4.3 nM 8.37
CHEMBL401830 IC50 = 4.6 nM 8.34
CHEMBL401988 IC50 = 5.2 nM 8.28
CHEMBL404638 IC50 = 5.8 nM 8.24
CHEMBL428951 IC50 = 7.7 nM 8.11
CHEMBL403758 IC50 = 9.0 nM 8.05
CHEMBL257985 IC50 = 12.0 nM 7.92
CHEMBL258165 IC50 = 13.0 nM 7.89
CHEMBL403944 IC50 = 15.0 nM 7.82
CHEMBL257364 IC50 = 20.0 nM 7.70
CHEMBL404564 IC50 = 21.0 nM 7.68
CHEMBL403369 IC50 = 26.0 nM 7.58
CHEMBL253953 IC50 = 27.0 nM 7.57
CHEMBL254993 IC50 = 28.0 nM 7.55
CHEMBL404743 IC50 = 28.0 nM 7.55
CHEMBL253955 IC50 = 32.0 nM 7.50
CHEMBL254790 IC50 = 34.0 nM 7.47
CHEMBL257962 IC50 = 38.0 nM 7.42
CHEMBL403549 IC50 = 43.0 nM 7.37
CHEMBL403589 IC50 = 50.0 nM 7.30
CHEMBL404173 IC50 = 88.0 nM 7.06
CHEMBL402302 IC50 = 89.0 nM 7.05
CHEMBL404880 IC50 = 89.0 nM 7.05
CHEMBL429318 IC50 = 90.0 nM 7.05
CHEMBL428429 FIG 1 IC50 = 109.0 nM 6.96
CHEMBL428430 IC50 = 200.0 nM 6.70
CHEMBL258217 IC50 = 250.0 nM 6.60
CHEMBL403384 IC50 = 260.0 nM 6.58
CHEMBL403165 IC50 = 630.0 nM 6.20
CHEMBL403687 IC50 = 963.0 nM 6.02
CHEMBL257753 IC50 < 1.0 nM -
CHEMBL257754 IC50 < 1.0 nM -
CHEMBL254789 IC50 < 1.0 nM -