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Assay Detail

CHEMBL855992

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Binding
Inhibition of human 11beta-HSD2
18
Total Activities
17
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

11-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL3746)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.
Yeh VS, Kurukulasuriya R, Madar D, Patel JR, Fung S, Monzon K, Chiou W, Wang J, Jacobson P, Sham HL, Link JT.
Bioorg Med Chem Lett (2006) 16 : 5408 -5413
PubMed 16890427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.25 4.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386315 1 4.80
CHEMBL3085038 1 4.16
CHEMBL218247 1 4.05
CHEMBL219606 1 4.00
CHEMBL384426 1 -
CHEMBL219403 2 -
CHEMBL216783 1 -
CHEMBL375743 1 -
CHEMBL384692 1 -
CHEMBL374409 1 -
CHEMBL218246 1 -
CHEMBL219448 1 -
CHEMBL219295 1 -
CHEMBL387010 1 -
CHEMBL386947 1 -
CHEMBL387424 1 -
CHEMBL376272 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386315 IC50 = 16000.0 nM 4.80
CHEMBL3085038 IC50 = 70000.0 nM 4.16
CHEMBL218247 IC50 = 90000.0 nM 4.05
CHEMBL219606 IC50 = 100000.0 nM 4.00
CHEMBL384426 IC50 > 30000.0 nM -
CHEMBL219403 IC50 > 30000.0 nM -
CHEMBL216783 IC50 > 30000.0 nM -
CHEMBL375743 IC50 > 30000.0 nM -
CHEMBL384692 IC50 - -
CHEMBL374409 IC50 > 100000.0 nM -
CHEMBL376272 IC50 > 100000.0 nM -
CHEMBL218246 IC50 > 30000.0 nM -
CHEMBL219295 IC50 > 100000.0 nM -
CHEMBL387010 IC50 > 100000.0 nM -
CHEMBL219403 IC50 > 100000.0 nM -
CHEMBL386947 IC50 - -
CHEMBL387424 IC50 - -
CHEMBL219448 IC50 > 100000.0 nM -