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Assay Detail

CHEMBL1827520

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Functional
Inhibition of Shh signaling in mouse Shh-light2 cells by Gli-dependent firefly luciferase reporter gene assay
ChEMBL ↗
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Shh Light II
Confidence 1 — Organism
Curated By Autocuration

Target

Shh Light II (CHEMBL3430862) ↗
Type CELL-LINE
Organism Mus musculus

Publication

Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.
Ontoria JM, Bufi LL, Torrisi C, Bresciani A, Giomini C, Rowley M, Serafini S, Bin H, Hao W, Steinkühler C, Jones P.
Bioorg Med Chem Lett (2011) 21 : 5274 -5282
PubMed 21803580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.25 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823863 — — 1 8.30
CHEMBL1822468 — — 1 8.30
CHEMBL1823865 — — 1 7.28
CHEMBL1823841 — — 1 7.24
CHEMBL1823861 — — 1 7.05
CHEMBL1823591 — — 1 6.85
CHEMBL1823833 — — 1 6.72
CHEMBL1823821 — — 1 6.60
CHEMBL1823862 — — 1 6.46
CHEMBL1823859 — — 1 6.44
CHEMBL1823839 — — 1 6.39
CHEMBL1823579 — — 1 6.39
CHEMBL1823825 — — 1 6.39
CHEMBL1823616 — — 1 6.37
CHEMBL1823828 — — 1 6.36
CHEMBL1823832 — — 1 6.32
CHEMBL1823854 — — 1 6.32
CHEMBL1823857 — — 1 6.30
CHEMBL1823584 — — 1 6.29
CHEMBL1823842 — — 1 6.24
CHEMBL1823840 — — 1 6.20
CHEMBL1823585 — — 1 6.17
CHEMBL1823831 — — 1 6.16
CHEMBL1823617 — — 1 6.08
CHEMBL1823858 — — 1 6.07
CHEMBL1823586 — — 1 6.05
CHEMBL1823590 — — 1 5.89
CHEMBL1823589 — — 1 5.89
CHEMBL1823834 — — 1 5.85
CHEMBL1823835 — — 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823863 — IC50 = 5.0 nM 8.30
CHEMBL1822468 — IC50 = 5.0 nM 8.30
CHEMBL1823865 — IC50 = 53.0 nM 7.28
CHEMBL1823841 — IC50 = 57.0 nM 7.24
CHEMBL1823861 — IC50 = 89.0 nM 7.05
CHEMBL1823591 — IC50 = 140.0 nM 6.85
CHEMBL1823833 — IC50 = 190.0 nM 6.72
CHEMBL1823821 — IC50 = 250.0 nM 6.60
CHEMBL1823862 — IC50 = 350.0 nM 6.46
CHEMBL1823859 — IC50 = 360.0 nM 6.44
CHEMBL1823825 — IC50 = 410.0 nM 6.39
CHEMBL1823579 — IC50 = 410.0 nM 6.39
CHEMBL1823839 — IC50 = 410.0 nM 6.39
CHEMBL1823616 — IC50 = 430.0 nM 6.37
CHEMBL1823828 — IC50 = 440.0 nM 6.36
CHEMBL1823832 — IC50 = 480.0 nM 6.32
CHEMBL1823854 — IC50 = 480.0 nM 6.32
CHEMBL1823857 — IC50 = 500.0 nM 6.30
CHEMBL1823584 — IC50 = 510.0 nM 6.29
CHEMBL1823842 — IC50 = 580.0 nM 6.24
CHEMBL1823840 — IC50 = 630.0 nM 6.20
CHEMBL1823585 — IC50 = 680.0 nM 6.17
CHEMBL1823831 — IC50 = 700.0 nM 6.16
CHEMBL1823617 — IC50 = 840.0 nM 6.08
CHEMBL1823858 — IC50 = 850.0 nM 6.07
CHEMBL1823586 — IC50 = 900.0 nM 6.05
CHEMBL1823590 — IC50 = 1300.0 nM 5.89
CHEMBL1823589 — IC50 = 1300.0 nM 5.89
CHEMBL1823834 — IC50 = 1400.0 nM 5.85
CHEMBL1823835 — IC50 = 1600.0 nM 5.80
CHEMBL1823836 — IC50 = 2000.0 nM 5.70
CHEMBL1823829 — IC50 = 2300.0 nM 5.64
CHEMBL1823587 — IC50 = 2400.0 nM 5.62
CHEMBL1823581 — IC50 = 2400.0 nM 5.62
CHEMBL1823855 — IC50 = 2500.0 nM 5.60
CHEMBL1823588 — IC50 = 2500.0 nM 5.60
CHEMBL1823853 — IC50 = 2700.0 nM 5.57
CHEMBL1823837 — IC50 = 2800.0 nM 5.55
CHEMBL1823838 — IC50 = 3000.0 nM 5.52
CHEMBL1823827 — IC50 = 3100.0 nM 5.51
CHEMBL1823856 — IC50 = 3200.0 nM 5.50
CHEMBL1823822 — IC50 > 2500.0 nM -