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Assay Detail

CHEMBL3784262

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Binding
Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 20mins before the addition of substrate by Ellman's method
ChEMBL ↗
72
Total Activities
50
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4078) ↗
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

Converting maslinic acid into an effective inhibitor of acylcholinesterases.
Schwarz S, Loesche A, Lucas SD, Sommerwerk S, Serbian I, Siewert B, Pianowski E, Csuk R.
Eur J Med Chem (2015) 103 : 438 -445
PubMed 26383128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 5.13 6.27
IC50 22 5.00 5.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1555 GALANTAMINE HYDROBROMIDE 4.0 1 6.27
CHEMBL3086609 — — 2 5.78
CHEMBL3781995 — — 2 5.69
CHEMBL3086607 — — 2 5.48
CHEMBL3086597 — — 2 5.46
CHEMBL3086615 — — 2 5.41
CHEMBL3086603 — — 2 5.39
CHEMBL3086612 — — 2 5.36
CHEMBL3086611 — — 2 5.24
CHEMBL3086605 — — 2 5.22
CHEMBL4299322 — — 2 5.21
CHEMBL3780430 — — 2 5.20
CHEMBL3779955 — — 1 5.19
CHEMBL3781136 — — 2 5.18
CHEMBL3086608 — — 2 5.17
CHEMBL3780423 — — 2 5.09
CHEMBL3086599 — — 2 5.06
CHEMBL3781812 — — 2 4.88
CHEMBL3086602 — — 2 4.86
CHEMBL3780432 — — 2 4.79
CHEMBL3086610 — — 2 4.75
CHEMBL3781042 — — 2 4.70
CHEMBL3325867 — — 2 4.69
CHEMBL3086604 — — 2 4.51
CHEMBL3086616 — — 1 -
CHEMBL3086601 — — 1 -
CHEMBL3781066 — — 1 -
CHEMBL3779951 — — 1 -
CHEMBL482673 AUGUSTIC ACID — 1 -
CHEMBL3086600 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1555 GALANTAMINE HYDROBROMIDE Ki = 540.0 nM 6.27
CHEMBL3086609 — Ki = 1680.0 nM 5.78
CHEMBL3781995 — Ki = 2030.0 nM 5.69
CHEMBL3086607 — Ki = 3310.0 nM 5.48
CHEMBL3086597 — Ki = 3490.0 nM 5.46
CHEMBL3086615 — IC50 = 3870.0 nM 5.41
CHEMBL3086603 — IC50 = 4070.0 nM 5.39
CHEMBL3086612 — IC50 = 4380.0 nM 5.36
CHEMBL3781995 — IC50 = 4630.0 nM 5.33
CHEMBL3086597 — IC50 = 4680.0 nM 5.33
CHEMBL3086612 — Ki = 4780.0 nM 5.32
CHEMBL3086611 — Ki = 5710.0 nM 5.24
CHEMBL3086605 — Ki = 6010.0 nM 5.22
CHEMBL4299322 — Ki = 6140.0 nM 5.21
CHEMBL3086607 — IC50 = 6250.0 nM 5.20
CHEMBL3780430 — Ki = 6250.0 nM 5.20
CHEMBL3779955 — Ki = 6490.0 nM 5.19
CHEMBL3781136 — IC50 = 6600.0 nM 5.18
CHEMBL3086611 — IC50 = 6570.0 nM 5.18
CHEMBL3086608 — Ki = 6760.0 nM 5.17
CHEMBL3781136 — Ki = 6850.0 nM 5.16
CHEMBL4299322 — IC50 = 7410.0 nM 5.13
CHEMBL3780423 — Ki = 8140.0 nM 5.09
CHEMBL3086603 — Ki = 8760.0 nM 5.06
CHEMBL3086599 — IC50 = 8760.0 nM 5.06
CHEMBL3086615 — Ki = 10020.0 nM 5.00
CHEMBL3086605 — IC50 = 10330.0 nM 4.99
CHEMBL3086609 — IC50 = 10450.0 nM 4.98
CHEMBL3086608 — IC50 = 11700.0 nM 4.93
CHEMBL3781812 — Ki = 13120.0 nM 4.88
CHEMBL3086602 — IC50 = 13760.0 nM 4.86
CHEMBL3780430 — IC50 = 15280.0 nM 4.82
CHEMBL3781812 — IC50 = 15140.0 nM 4.82
CHEMBL3780423 — IC50 = 15080.0 nM 4.82
CHEMBL3780432 — Ki = 16190.0 nM 4.79
CHEMBL3086599 — Ki = 16860.0 nM 4.77
CHEMBL3086610 — IC50 = 17580.0 nM 4.75
CHEMBL3086602 — Ki = 20120.0 nM 4.70
CHEMBL3781042 — IC50 = 20000.0 nM 4.70
CHEMBL3325867 — Ki = 20530.0 nM 4.69
CHEMBL3325867 — IC50 = 21270.0 nM 4.67
CHEMBL3086610 — Ki = 22480.0 nM 4.65
CHEMBL3781042 — Ki = 25140.0 nM 4.60
CHEMBL3780432 — IC50 = 29360.0 nM 4.53
CHEMBL3086604 — IC50 = 31180.0 nM 4.51
CHEMBL3086604 — Ki = 34850.0 nM 4.46
CHEMBL508614 — Ki > 10000.0 nM -
CHEMBL3086601 — Ki > 10000.0 nM -
CHEMBL3086600 — Ki > 30000.0 nM -
CHEMBL204906 — Ki > 100000.0 nM -