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Assay Detail

CHEMBL816914

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Binding
In vitro binding affinity to vesamicol receptor using [3H]vesamicol.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vesicular acetylcholine transporter (CHEMBL3313)
Type SINGLE PROTEIN
Organism Torpedo californica

Publication

Spirovesamicols: conformationally restricted analogs of 2-(4-phenylpiperidino)cyclohexanol (vesamicol, AH5183) as potential modulators of presynaptic cholinergic function.
Efange SM, Khare AB, Foulon C, Akella SK, Parsons SM.
J Med Chem (1994) 37 : 2574 -2582
PubMed 8057300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 9.16 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86366 1 10.30
CHEMBL87379 BENZOVESAMICOL 1 10.26
CHEMBL50880 1 10.20
CHEMBL87595 1 9.92
CHEMBL313710 1 9.83
CHEMBL314848 1 9.67
CHEMBL87693 1 9.61
CHEMBL86983 1 9.58
CHEMBL431223 1 9.57
CHEMBL87414 1 9.44
CHEMBL87594 1 9.44
CHEMBL406130 1 9.39
CHEMBL87232 1 9.20
CHEMBL314170 1 9.18
CHEMBL88046 1 9.12
CHEMBL314687 1 9.10
CHEMBL87214 1 9.10
CHEMBL315226 1 9.07
CHEMBL431413 1 9.01
CHEMBL20730 VESAMICOL 1 9.00
CHEMBL424241 1 8.85
CHEMBL86816 1 8.58
CHEMBL84738 1 8.24
CHEMBL87287 1 8.16
CHEMBL315146 1 8.12
CHEMBL87435 1 7.74
CHEMBL87652 1 7.62
CHEMBL87381 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86366 Ki = 0.05 nM 10.30
CHEMBL87379 BENZOVESAMICOL Ki = 0.055 nM 10.26
CHEMBL50880 Ki = 0.063 nM 10.20
CHEMBL87595 Ki = 0.121 nM 9.92
CHEMBL313710 Ki = 0.147 nM 9.83
CHEMBL314848 Ki = 0.212 nM 9.67
CHEMBL87693 Ki = 0.248 nM 9.61
CHEMBL86983 Ki = 0.264 nM 9.58
CHEMBL431223 Ki = 0.271 nM 9.57
CHEMBL87414 Ki = 0.36 nM 9.44
CHEMBL87594 Ki = 0.36 nM 9.44
CHEMBL406130 Ki = 0.41 nM 9.39
CHEMBL87232 Ki = 0.638 nM 9.20
CHEMBL314170 Ki = 0.66 nM 9.18
CHEMBL88046 Ki = 0.762 nM 9.12
CHEMBL314687 Ki = 0.8 nM 9.10
CHEMBL87214 Ki = 0.798 nM 9.10
CHEMBL315226 Ki = 0.856 nM 9.07
CHEMBL431413 Ki = 0.98 nM 9.01
CHEMBL20730 VESAMICOL Ki = 1.0 nM 9.00
CHEMBL424241 Ki = 1.4 nM 8.85
CHEMBL86816 Ki = 2.638 nM 8.58
CHEMBL84738 Ki = 5.8 nM 8.24
CHEMBL87287 Ki = 6.93 nM 8.16
CHEMBL315146 Ki = 7.59 nM 8.12
CHEMBL87435 Ki = 18.36 nM 7.74
CHEMBL87652 Ki = 24.25 nM 7.62
CHEMBL87381 Ki = 0.0065 nM -