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Assay Detail

CHEMBL3369133

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Binding
Inhibition of equine serum BChE
ChEMBL ↗
76
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Equus caballus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763) ↗
Type SINGLE PROTEIN
Organism Equus caballus

Publication

Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode.
Darras FH, Wehle S, Huang G, Sotriffer CA, Decker M.
Bioorg Med Chem (2014) 22 : 4867 -4881
PubMed 25047936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 76 5.44 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 2 8.44
CHEMBL3323020 — — 2 6.23
CHEMBL3323057 — — 2 6.11
CHEMBL3323056 — — 2 6.08
CHEMBL3323047 — — 2 6.06
CHEMBL3323042 — — 2 6.02
CHEMBL3323021 — — 2 6.02
CHEMBL3323040 — — 2 5.76
CHEMBL3323060 — — 2 5.75
CHEMBL3323066 — — 2 5.75
CHEMBL3323044 — — 2 5.74
CHEMBL3323050 — — 2 5.74
CHEMBL3323039 — — 2 5.73
CHEMBL3323037 — — 2 5.73
CHEMBL3323043 — — 2 5.67
CHEMBL3323038 — — 2 5.62
CHEMBL3323046 — — 2 5.57
CHEMBL3323069 — — 2 5.52
CHEMBL3323048 — — 2 5.44
CHEMBL3323036 — — 2 5.38
CHEMBL3323049 — — 2 5.29
CHEMBL3323054 — — 2 5.28
CHEMBL3323063 — — 2 5.26
CHEMBL3323059 — — 2 5.18
CHEMBL3323071 — — 2 5.07
CHEMBL3323045 — — 2 5.06
CHEMBL3323062 — — 2 5.04
CHEMBL3323041 — — 2 5.04
CHEMBL3323055 — — 2 4.98
CHEMBL3323068 — — 2 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 3.664 nM 8.44
CHEMBL95 TACRINE IC50 = 3.7 nM 8.43
CHEMBL3323020 — IC50 = 584.79 nM 6.23
CHEMBL3323020 — IC50 = 584.0 nM 6.23
CHEMBL3323057 — IC50 = 776.0 nM 6.11
CHEMBL3323057 — IC50 = 776.25 nM 6.11
CHEMBL3323056 — IC50 = 829.0 nM 6.08
CHEMBL3323056 — IC50 = 827.94 nM 6.08
CHEMBL3323047 — IC50 = 864.97 nM 6.06
CHEMBL3323047 — IC50 = 865.0 nM 6.06
CHEMBL3323021 — IC50 = 955.0 nM 6.02
CHEMBL3323042 — IC50 = 955.0 nM 6.02
CHEMBL3323042 — IC50 = 954.99 nM 6.02
CHEMBL3323040 — IC50 = 1730.0 nM 5.76
CHEMBL3323040 — IC50 = 1725.84 nM 5.76
CHEMBL3323066 — IC50 = 1800.0 nM 5.75
CHEMBL3323060 — IC50 = 1770.0 nM 5.75
CHEMBL3323050 — IC50 = 1840.0 nM 5.74
CHEMBL3323050 — IC50 = 1840.77 nM 5.74
CHEMBL3323066 — IC50 = 1803.02 nM 5.74
CHEMBL3323044 — IC50 = 1830.0 nM 5.74
CHEMBL3323044 — IC50 = 1832.31 nM 5.74
CHEMBL3323037 — IC50 = 1870.0 nM 5.73
CHEMBL3323039 — IC50 = 1880.0 nM 5.73
CHEMBL3323039 — IC50 = 1879.32 nM 5.73
CHEMBL3323037 — IC50 = 1874.99 nM 5.73
CHEMBL3323043 — IC50 = 2160.0 nM 5.67
CHEMBL3323043 — IC50 = 2157.74 nM 5.67
CHEMBL3323038 — IC50 = 2400.0 nM 5.62
CHEMBL3323038 — IC50 = 2398.83 nM 5.62
CHEMBL3323046 — IC50 = 2673.01 nM 5.57
CHEMBL3323060 — IC50 = 2673.01 nM 5.57
CHEMBL3323046 — IC50 = 2670.0 nM 5.57
CHEMBL3323069 — IC50 = 3030.0 nM 5.52
CHEMBL3323069 — IC50 = 3026.91 nM 5.52
CHEMBL3323048 — IC50 = 3605.79 nM 5.44
CHEMBL3323048 — IC50 = 3610.0 nM 5.44
CHEMBL3323036 — IC50 = 4140.0 nM 5.38
CHEMBL3323049 — IC50 = 5100.0 nM 5.29
CHEMBL3323049 — IC50 = 5093.31 nM 5.29
CHEMBL3323054 — IC50 = 5223.96 nM 5.28
CHEMBL3323054 — IC50 = 5220.0 nM 5.28
CHEMBL3323063 — IC50 = 5482.77 nM 5.26
CHEMBL3323063 — IC50 = 5490.0 nM 5.26
CHEMBL3323059 — IC50 = 6546.36 nM 5.18
CHEMBL3323059 — IC50 = 6550.0 nM 5.18
CHEMBL3323071 — IC50 = 8511.38 nM 5.07
CHEMBL3323071 — IC50 = 8600.0 nM 5.07
CHEMBL3323045 — IC50 = 8689.6 nM 5.06
CHEMBL3323045 — IC50 = 8680.0 nM 5.06