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Assay Detail

CHEMBL636849

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

Binding
Inhibition of active transport of [3H]acetylcholine using purified Torpedo californica synaptic vesicles
ChEMBL ↗
87
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo californica
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Vesicular acetylcholine transporter (CHEMBL4767) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogues of trans-2-(4-phenylpiperidino)cyclohexanol (vesamicol).
Rogers GA, Parsons SM, Anderson DC, Nilsson LM, Bahr BA, Kornreich WD, Kaufman R, Jacobs RS, Kirtman B.
J Med Chem (1989) 32 : 1217 -1230
PubMed 2724295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 87 6.15 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20721 — — 2 8.00
CHEMBL20463 — — 1 7.70
CHEMBL20730 VESAMICOL — 1 7.70
CHEMBL21309 — — 1 7.40
CHEMBL20943 — — 2 7.40
CHEMBL21271 — — 1 7.30
CHEMBL21151 — — 1 7.30
CHEMBL20382 — — 1 7.30
CHEMBL20499 — — 1 7.30
CHEMBL21243 — — 1 7.16
CHEMBL21722 — — 1 7.05
CHEMBL20881 — — 1 7.00
CHEMBL278303 — — 1 7.00
CHEMBL277630 — — 1 7.00
CHEMBL20481 — — 1 7.00
CHEMBL21165 — — 1 7.00
CHEMBL282894 — — 1 7.00
CHEMBL20479 — — 1 7.00
CHEMBL281595 — — 1 7.00
CHEMBL20431 — — 1 6.70
CHEMBL277033 — — 1 6.70
CHEMBL20429 — — 1 6.70
CHEMBL266183 — — 1 6.70
CHEMBL278834 — — 1 6.70
CHEMBL20720 — — 1 6.70
CHEMBL21152 — — 2 6.70
CHEMBL22052 — — 1 6.52
CHEMBL416916 — — 1 6.52
CHEMBL283140 — — 1 6.52
CHEMBL20689 — — 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20721 — IC50 = 10.0 nM 8.00
CHEMBL20463 — IC50 = 20.0 nM 7.70
CHEMBL20730 VESAMICOL IC50 = 20.0 nM 7.70
CHEMBL21309 — IC50 = 40.0 nM 7.40
CHEMBL20943 — IC50 = 40.0 nM 7.40
CHEMBL21271 — IC50 = 50.0 nM 7.30
CHEMBL21151 — IC50 = 50.0 nM 7.30
CHEMBL20382 — IC50 = 50.0 nM 7.30
CHEMBL20499 — IC50 = 50.0 nM 7.30
CHEMBL20721 — IC50 = 60.0 nM 7.22
CHEMBL21243 — IC50 = 70.0 nM 7.16
CHEMBL21722 — IC50 = 90.0 nM 7.05
CHEMBL21165 — IC50 = 100.0 nM 7.00
CHEMBL20479 — IC50 = 100.0 nM 7.00
CHEMBL282894 — IC50 = 100.0 nM 7.00
CHEMBL281595 — IC50 = 100.0 nM 7.00
CHEMBL20881 — IC50 = 100.0 nM 7.00
CHEMBL20481 — IC50 = 100.0 nM 7.00
CHEMBL277630 — IC50 = 100.0 nM 7.00
CHEMBL278303 — IC50 = 100.0 nM 7.00
CHEMBL20720 — IC50 = 200.0 nM 6.70
CHEMBL278834 — IC50 = 200.0 nM 6.70
CHEMBL21152 — IC50 = 200.0 nM 6.70
CHEMBL20429 — IC50 = 200.0 nM 6.70
CHEMBL277033 — IC50 = 200.0 nM 6.70
CHEMBL20431 — IC50 = 200.0 nM 6.70
CHEMBL266183 — IC50 = 200.0 nM 6.70
CHEMBL283140 — IC50 = 300.0 nM 6.52
CHEMBL21152 — IC50 = 300.0 nM 6.52
CHEMBL21148 — IC50 = 300.0 nM 6.52
CHEMBL20664 — IC50 = 300.0 nM 6.52
CHEMBL20928 — IC50 = 300.0 nM 6.52
CHEMBL416916 — IC50 = 300.0 nM 6.52
CHEMBL279485 — IC50 = 300.0 nM 6.52
CHEMBL22052 — IC50 = 300.0 nM 6.52
CHEMBL20719 — IC50 = 300.0 nM 6.52
CHEMBL278382 — IC50 = 300.0 nM 6.52
CHEMBL20689 — IC50 = 300.0 nM 6.52
CHEMBL20491 — IC50 = 400.0 nM 6.40
CHEMBL20744 — IC50 = 500.0 nM 6.30
CHEMBL20657 — IC50 = 500.0 nM 6.30
CHEMBL417277 — IC50 = 500.0 nM 6.30
CHEMBL277861 — IC50 = 500.0 nM 6.30
CHEMBL20593 — IC50 = 600.0 nM 6.22
CHEMBL21375 — IC50 = 800.0 nM 6.10
CHEMBL20502 — IC50 = 800.0 nM 6.10
CHEMBL2079585 — IC50 = 1000.0 nM 6.00
CHEMBL280364 — IC50 = 1000.0 nM 6.00
CHEMBL20772 — IC50 = 1000.0 nM 6.00
CHEMBL20601 — IC50 = 1000.0 nM 6.00