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Assay Detail

CHEMBL2033031

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

Functional
Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Shh Light II
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein smoothened (CHEMBL5971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity.
Solinas A, Faure H, Roudaut H, Traiffort E, Schoenfelder A, Mann A, Manetti F, Taddei M, Ruat M.
J Med Chem (2012) 55 : 1559 -1571
PubMed 22268551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 6.87 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473417 VISMODEGIB 4.0 1 8.15
CHEMBL2031277 1 7.89
CHEMBL2031288 1 7.85
CHEMBL2031290 1 7.82
CHEMBL2031263 1 7.54
CHEMBL2031287 1 7.48
CHEMBL2031268 1 7.39
CHEMBL2031289 1 7.16
CHEMBL2031283 1 7.16
CHEMBL2031077 1 7.10
CHEMBL2031098 1 7.05
CHEMBL2031245 1 7.00
CHEMBL2031291 1 6.96
CHEMBL2031281 1 6.96
CHEMBL2031267 1 6.89
CHEMBL480889 1 6.85
CHEMBL2031273 1 6.80
CHEMBL2031295 1 6.80
CHEMBL2031253 1 6.75
CHEMBL2031294 1 6.72
CHEMBL2031258 1 6.72
CHEMBL2031284 1 6.66
CHEMBL2031282 1 6.54
CHEMBL254129 CYCLOPAMINE 1 6.52
CHEMBL2031292 1 6.43
CHEMBL2031080 1 6.28
CHEMBL2031285 1 6.19
CHEMBL2031084 1 6.19
CHEMBL2031254 1 6.09
CHEMBL2031286 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473417 VISMODEGIB IC50 = 7.0 nM 8.15
CHEMBL2031277 IC50 = 13.0 nM 7.89
CHEMBL2031288 IC50 = 14.0 nM 7.85
CHEMBL2031290 IC50 = 15.0 nM 7.82
CHEMBL2031263 IC50 = 29.0 nM 7.54
CHEMBL2031287 IC50 = 33.0 nM 7.48
CHEMBL2031268 IC50 = 41.0 nM 7.39
CHEMBL2031289 IC50 = 70.0 nM 7.16
CHEMBL2031283 IC50 = 70.0 nM 7.16
CHEMBL2031077 IC50 = 80.0 nM 7.10
CHEMBL2031098 IC50 = 90.0 nM 7.05
CHEMBL2031245 IC50 = 100.0 nM 7.00
CHEMBL2031291 IC50 = 110.0 nM 6.96
CHEMBL2031281 IC50 = 110.0 nM 6.96
CHEMBL2031267 IC50 = 130.0 nM 6.89
CHEMBL480889 IC50 = 140.0 nM 6.85
CHEMBL2031273 IC50 = 160.0 nM 6.80
CHEMBL2031295 IC50 = 160.0 nM 6.80
CHEMBL2031253 IC50 = 180.0 nM 6.75
CHEMBL2031294 IC50 = 190.0 nM 6.72
CHEMBL2031258 IC50 = 190.0 nM 6.72
CHEMBL2031284 IC50 = 220.0 nM 6.66
CHEMBL2031282 IC50 = 290.0 nM 6.54
CHEMBL254129 CYCLOPAMINE IC50 = 300.0 nM 6.52
CHEMBL2031292 IC50 = 370.0 nM 6.43
CHEMBL2031080 IC50 = 520.0 nM 6.28
CHEMBL2031084 IC50 = 650.0 nM 6.19
CHEMBL2031285 IC50 = 640.0 nM 6.19
CHEMBL2031254 IC50 = 820.0 nM 6.09
CHEMBL2031286 IC50 = 900.0 nM 6.05
CHEMBL2031256 IC50 = 1100.0 nM 5.96
CHEMBL2031079 IC50 = 1800.0 nM 5.75
CHEMBL2031096 IC50 - -
CHEMBL2031097 IC50 - -
CHEMBL2031244 IC50 - -
CHEMBL2031081 IC50 - -
CHEMBL2031246 IC50 - -
CHEMBL2031257 IC50 - -
CHEMBL2031248 IC50 - -
CHEMBL2031082 IC50 - -
CHEMBL2031249 IC50 - -
CHEMBL2031250 IC50 - -
CHEMBL2031251 IC50 - -
CHEMBL2031252 IC50 - -
CHEMBL2031083 IC50 - -
CHEMBL2031255 IC50 - -
CHEMBL2031247 IC50 - -
CHEMBL2031279 IC50 - -
CHEMBL2031280 IC50 - -
CHEMBL2031278 IC50 - -