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Assay Detail

CHEMBL987095

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

Functional
Inhibition of Hedgehog pathway-dependent oxysterol-induced mouse C3 H10T1/2 cell differentiation assessed as alkaline phosphatase production after 72 hrs
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type C3H 10T1/2
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Publication

Semisynthetic cyclopamine analogues as potent and orally bioavailable hedgehog pathway antagonists.
Tremblay MR, Nevalainen M, Nair SJ, Porter JR, Castro AC, Behnke ML, Yu LC, Hagel M, White K, Faia K, Grenier L, Campbell MJ, Cushing J, Woodward CN, Hoyt J, Foley MA, Read MA, Sydor JR, Tong JK, Palombella VJ, McGovern K, Adams J.
J Med Chem (2008) 51 : 6646 -6649
PubMed 18842035 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 6.87 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL449569 1 8.00
CHEMBL506708 1 7.70
CHEMBL489867 1 6.92
CHEMBL254129 CYCLOPAMINE 1 6.77
CHEMBL473393 1 6.70
CHEMBL509596 1 6.40
CHEMBL483601 1 6.40
CHEMBL483765 1 6.10
CHEMBL504507 1 -
CHEMBL451346 1 -
CHEMBL490068 1 -
CHEMBL519497 1 -
CHEMBL483591 CYCLOPROPYL CYCLOPAMINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL449569 EC50 = 10.0 nM 8.00
CHEMBL506708 EC50 = 20.0 nM 7.70
CHEMBL489867 EC50 = 120.0 nM 6.92
CHEMBL254129 CYCLOPAMINE EC50 = 170.0 nM 6.77
CHEMBL473393 EC50 = 200.0 nM 6.70
CHEMBL509596 EC50 = 400.0 nM 6.40
CHEMBL483601 EC50 = 400.0 nM 6.40
CHEMBL483765 EC50 = 800.0 nM 6.10
CHEMBL504507 EC50 > 2000.0 nM -
CHEMBL451346 EC50 > 1000.0 nM -
CHEMBL490068 EC50 > 2500.0 nM -
CHEMBL519497 EC50 > 2500.0 nM -
CHEMBL483591 CYCLOPROPYL CYCLOPAMINE EC50 > 2000.0 nM -