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Assay Detail

CHEMBL3222359

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

Binding
Inhibition of Torpedo californica eel AChE using acetylthiocholine/DTNB as substrate preincubated for 10 mins followed by substrate addition measured every 30 secs for 30 mins by Ellmans method
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo californica
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4780)
Type SINGLE PROTEIN
Organism Torpedo californica

Publication

Tacrine-mefenamic acid hybrids for inhibition of acetylcholinesterase
Bornstein JJ, Eckroat TJ, Houghton JL, Jones CK, Green KD, Garneau-Tsodikova S
Medchemcomm (2011) 2 : 406 -412
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 7.46 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3221566 1 9.38
CHEMBL2393227 1 9.30
CHEMBL2393229 1 9.11
CHEMBL2393109 1 8.94
CHEMBL3221006 1 8.86
CHEMBL3221008 1 8.81
CHEMBL3221292 1 8.78
CHEMBL3221005 1 8.65
CHEMBL2393111 1 8.53
CHEMBL3221286 1 8.48
CHEMBL3221285 1 8.44
CHEMBL278020 NEOSTIGMINE 4.0 1 8.34
CHEMBL3221282 1 8.26
CHEMBL2393224 1 8.18
CHEMBL2393228 1 8.16
CHEMBL3217792 1 8.15
CHEMBL3221565 1 8.12
CHEMBL2393225 1 8.10
CHEMBL3221284 1 8.09
CHEMBL3221287 1 8.07
CHEMBL2393226 1 7.96
CHEMBL2393106 1 7.87
CHEMBL3221283 1 7.86
CHEMBL3221569 1 7.77
CHEMBL3221288 1 7.76
CHEMBL3221278 1 7.74
CHEMBL3221568 1 7.74
CHEMBL3221289 1 7.73
CHEMBL3221291 1 7.69
CHEMBL3221290 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3221566 IC50 = 0.418 nM 9.38
CHEMBL2393227 IC50 = 0.495 nM 9.30
CHEMBL2393229 IC50 = 0.776 nM 9.11
CHEMBL2393109 IC50 = 1.14 nM 8.94
CHEMBL3221006 IC50 = 1.39 nM 8.86
CHEMBL3221008 IC50 = 1.54 nM 8.81
CHEMBL3221292 IC50 = 1.65 nM 8.78
CHEMBL3221005 IC50 = 2.24 nM 8.65
CHEMBL2393111 IC50 = 2.94 nM 8.53
CHEMBL3221286 IC50 = 3.3 nM 8.48
CHEMBL3221285 IC50 = 3.6 nM 8.44
CHEMBL278020 NEOSTIGMINE IC50 = 4.6 nM 8.34
CHEMBL3221282 IC50 = 5.55 nM 8.26
CHEMBL2393224 IC50 = 6.67 nM 8.18
CHEMBL2393228 IC50 = 6.94 nM 8.16
CHEMBL3217792 IC50 = 7.13 nM 8.15
CHEMBL3221565 IC50 = 7.65 nM 8.12
CHEMBL2393225 IC50 = 7.91 nM 8.10
CHEMBL3221284 IC50 = 8.09 nM 8.09
CHEMBL3221287 IC50 = 8.58 nM 8.07
CHEMBL2393226 IC50 = 11.1 nM 7.96
CHEMBL2393106 IC50 = 13.6 nM 7.87
CHEMBL3221283 IC50 = 13.9 nM 7.86
CHEMBL3221569 IC50 = 17.0 nM 7.77
CHEMBL3221288 IC50 = 17.4 nM 7.76
CHEMBL3221278 IC50 = 18.3 nM 7.74
CHEMBL3221568 IC50 = 18.3 nM 7.74
CHEMBL3221289 IC50 = 18.7 nM 7.73
CHEMBL3221291 IC50 = 20.3 nM 7.69
CHEMBL3221290 IC50 = 28.1 nM 7.55
CHEMBL2393107 IC50 = 37.4 nM 7.43
CHEMBL3221567 IC50 = 39.8 nM 7.40
CHEMBL2393110 IC50 = 41.7 nM 7.38
CHEMBL3221010 IC50 = 50.9 nM 7.29
CHEMBL95 TACRINE IC50 = 52.4 nM 7.28
CHEMBL3221007 IC50 = 75.5 nM 7.12
CHEMBL3221570 IC50 = 80.1 nM 7.10
CHEMBL1115 PYRIDOSTIGMINE IC50 = 82.0 nM 7.09
CHEMBL3221270 IC50 = 87.3 nM 7.06
CHEMBL3221276 IC50 = 89.7 nM 7.05
CHEMBL3221293 IC50 = 156.0 nM 6.81
CHEMBL3221280 IC50 = 195.0 nM 6.71
CHEMBL3221274 IC50 = 262.0 nM 6.58
CHEMBL3221009 IC50 = 385.0 nM 6.42
CHEMBL3221275 IC50 = 426.0 nM 6.37
CHEMBL3221273 IC50 = 811.0 nM 6.09
CHEMBL3221279 IC50 = 985.0 nM 6.01
CHEMBL2390978 IC50 = 1380.0 nM 5.86
CHEMBL3221281 IC50 = 1440.0 nM 5.84
CHEMBL3221277 IC50 = 1860.0 nM 5.73