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Assay Detail

CHEMBL1687386

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Binding
Inhibition of squalene synthase
ChEMBL ↗
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Squalene synthase (CHEMBL3338) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new 2-aminobenzhydrol template for highly potent squalene synthase inhibitors.
Ichikawa M, Yokomizo A, Itoh M, Usui H, Shimizu H, Suzuki M, Terayama K, Kanda A, Sugita K.
Bioorg Med Chem (2011) 19 : 1930 -1949
PubMed 21353782 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 7.59 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1684849 — — 1 9.35
CHEMBL1684826 — — 1 9.07
CHEMBL1684999 — — 1 8.96
CHEMBL1684996 — — 1 8.96
CHEMBL1684838 — — 1 8.96
CHEMBL1685008 — — 1 8.89
CHEMBL1684829 — — 1 8.89
CHEMBL1685025 — — 1 8.89
CHEMBL1684833 — — 1 8.80
CHEMBL1685014 — — 1 8.77
CHEMBL1685028 — — 1 8.70
CHEMBL1684994 — — 1 8.70
CHEMBL1684837 — — 1 8.64
CHEMBL1684831 — — 1 8.62
CHEMBL1685005 — — 1 8.59
CHEMBL1685017 — — 1 8.55
CHEMBL1684832 — — 1 8.43
CHEMBL1685029 — — 1 8.17
CHEMBL1685018 — — 1 8.15
CHEMBL1684993 — — 1 8.14
CHEMBL1684841 — — 1 8.10
CHEMBL1685022 — — 1 8.08
CHEMBL1685000 — — 1 8.00
CHEMBL1685009 — — 1 7.89
CHEMBL1685011 — — 1 7.77
CHEMBL1684835 — — 1 7.70
CHEMBL1685002 — — 1 7.55
CHEMBL1684828 — — 1 7.01
CHEMBL1684827 — — 1 6.89
CHEMBL1685023 — — 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1684849 — IC50 = 0.45 nM 9.35
CHEMBL1684826 — IC50 = 0.85 nM 9.07
CHEMBL1684996 — IC50 = 1.1 nM 8.96
CHEMBL1684838 — IC50 = 1.1 nM 8.96
CHEMBL1684999 — IC50 = 1.1 nM 8.96
CHEMBL1685008 — IC50 = 1.3 nM 8.89
CHEMBL1684829 — IC50 = 1.3 nM 8.89
CHEMBL1685025 — IC50 = 1.3 nM 8.89
CHEMBL1684833 — IC50 = 1.6 nM 8.80
CHEMBL1685014 — IC50 = 1.7 nM 8.77
CHEMBL1685028 — IC50 = 2.0 nM 8.70
CHEMBL1684994 — IC50 = 2.0 nM 8.70
CHEMBL1684837 — IC50 = 2.3 nM 8.64
CHEMBL1684831 — IC50 = 2.4 nM 8.62
CHEMBL1685005 — IC50 = 2.6 nM 8.59
CHEMBL1685017 — IC50 = 2.8 nM 8.55
CHEMBL1684832 — IC50 = 3.7 nM 8.43
CHEMBL1685029 — IC50 = 6.8 nM 8.17
CHEMBL1685018 — IC50 = 7.0 nM 8.15
CHEMBL1684993 — IC50 = 7.2 nM 8.14
CHEMBL1684841 — IC50 = 7.9 nM 8.10
CHEMBL1685022 — IC50 = 8.4 nM 8.08
CHEMBL1685000 — IC50 = 10.0 nM 8.00
CHEMBL1685009 — IC50 = 13.0 nM 7.89
CHEMBL1685011 — IC50 = 17.0 nM 7.77
CHEMBL1684835 — IC50 = 20.0 nM 7.70
CHEMBL1685002 — IC50 = 28.0 nM 7.55
CHEMBL1684828 — IC50 = 97.0 nM 7.01
CHEMBL1684827 — IC50 = 130.0 nM 6.89
CHEMBL1685023 — IC50 = 190.0 nM 6.72
CHEMBL1684997 — IC50 = 210.0 nM 6.68
CHEMBL1684836 — IC50 = 220.0 nM 6.66
CHEMBL1684840 — IC50 = 260.0 nM 6.58
CHEMBL1684830 — IC50 = 280.0 nM 6.55
CHEMBL1685021 — IC50 = 290.0 nM 6.54
CHEMBL1684998 — IC50 = 410.0 nM 6.39
CHEMBL1684834 — IC50 = 410.0 nM 6.39
CHEMBL1684845 — IC50 = 600.0 nM 6.22
CHEMBL1684846 — IC50 = 650.0 nM 6.19
CHEMBL1684848 — IC50 = 770.0 nM 6.11
CHEMBL1684824 — IC50 = 1700.0 nM 5.77
CHEMBL1685010 — IC50 = 1700.0 nM 5.77
CHEMBL1684839 — IC50 = 2100.0 nM 5.68
CHEMBL1684825 — IC50 = 6500.0 nM 5.19
CHEMBL1684844 — IC50 = 21000.0 nM 4.68
CHEMBL1685006 — IC50 > 600.0 nM -
CHEMBL1684995 — IC50 > 600.0 nM -
CHEMBL1685001 — IC50 > 600.0 nM -
CHEMBL1685027 — IC50 > 600.0 nM -
CHEMBL1685026 — IC50 > 600.0 nM -