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Assay Detail

CHEMBL987100

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

Binding
Inhibition of GLI1-mediated transcriptional activity in human HaCaT cells by luciferase based reporter gene assay
8
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Zinc finger protein GLI1 (CHEMBL5461)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Hedgehog/GLI-mediated transcriptional inhibitors from Zizyphus cambodiana.
Arai MA, Tateno C, Hosoya T, Koyano T, Kowithayakorn T, Ishibashi M.
Bioorg Med Chem (2008) 16 : 9420 -9424
PubMed 18842418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.43 4.50
Activity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269277 BETULINIC ACID 1.0 2 4.50
CHEMBL470503 COLUBRINIC ACID 2 4.42
CHEMBL511805 ALPHITOLIC ACID 2 4.38
CHEMBL491069 CEANOTHIC ACID 1 -
CHEMBL522108 CEANOTHANOLIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269277 BETULINIC ACID IC50 = 32000.0 nM 4.50
CHEMBL470503 COLUBRINIC ACID IC50 = 38000.0 nM 4.42
CHEMBL511805 ALPHITOLIC ACID IC50 = 42000.0 nM 4.38
CHEMBL491069 CEANOTHIC ACID IC50 > 200000.0 nM -
CHEMBL522108 CEANOTHANOLIC ACID IC50 = 133000.0 nM -
CHEMBL470503 COLUBRINIC ACID Activity - -
CHEMBL269277 BETULINIC ACID Activity - -
CHEMBL511805 ALPHITOLIC ACID Activity - -