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Assay Detail

CHEMBL4825145

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

Binding
Inhibition of recombinant equine BChE by Ellman's method
26
Total Activities
26
Compounds Tested
2
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

Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors.
Schwarthoff S, Tischer N, Sager H, Schätz B, Rohrbach MM, Raztsou I, Robaa D, Gaube F, Arndt HD, Winckler T.
Bioorg Med Chem (2021) 46 : 116355 -116355
PubMed 34391122 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.38 8.10
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4848411 1 8.10
CHEMBL4864593 1 8.10
CHEMBL4850804 1 7.96
CHEMBL4855045 1 7.80
CHEMBL4873748 1 7.50
CHEMBL4874126 1 7.50
CHEMBL4850585 1 7.43
CHEMBL4878924 1 7.39
CHEMBL4870561 1 7.39
CHEMBL4860501 1 6.77
CHEMBL4863376 1 6.26
CHEMBL596112 1 6.05
CHEMBL12540 1 5.92
CHEMBL502 DONEPEZIL 4.0 1 5.89
CHEMBL261855 1 5.85
CHEMBL4856643 1 5.85
CHEMBL4850464 1 5.72
CHEMBL4859070 1 5.68
CHEMBL4849276 1 5.57
CHEMBL4865927 1 5.26
CHEMBL4849640 1 5.20
CHEMBL1712867 1 5.19
CHEMBL1984135 1 5.19
CHEMBL4857977 1 5.01
CHEMBL4846730 1 4.90
CHEMBL807 MEMANTINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4848411 IC50 = 8.0 nM 8.10
CHEMBL4864593 IC50 = 8.0 nM 8.10
CHEMBL4850804 IC50 = 11.0 nM 7.96
CHEMBL4855045 IC50 = 16.0 nM 7.80
CHEMBL4873748 IC50 = 32.0 nM 7.50
CHEMBL4874126 IC50 = 32.0 nM 7.50
CHEMBL4850585 IC50 = 37.0 nM 7.43
CHEMBL4878924 IC50 = 41.0 nM 7.39
CHEMBL4870561 IC50 = 41.0 nM 7.39
CHEMBL4860501 IC50 = 170.0 nM 6.77
CHEMBL4863376 IC50 = 550.0 nM 6.26
CHEMBL596112 IC50 = 890.0 nM 6.05
CHEMBL12540 IC50 = 1200.0 nM 5.92
CHEMBL502 DONEPEZIL IC50 = 1300.0 nM 5.89
CHEMBL261855 IC50 = 1400.0 nM 5.85
CHEMBL4856643 IC50 = 1400.0 nM 5.85
CHEMBL4850464 IC50 = 1900.0 nM 5.72
CHEMBL4859070 IC50 = 2100.0 nM 5.68
CHEMBL4849276 IC50 = 2700.0 nM 5.57
CHEMBL4865927 IC50 = 5500.0 nM 5.26
CHEMBL4849640 IC50 = 6300.0 nM 5.20
CHEMBL1712867 IC50 = 6500.0 nM 5.19
CHEMBL1984135 IC50 = 6500.0 nM 5.19
CHEMBL4857977 IC50 = 9800.0 nM 5.01
CHEMBL4846730 IC50 = 12600.0 nM 4.90
CHEMBL807 MEMANTINE Inhibition < 50.0 % -