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Assay Detail

CHEMBL753472

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Functional
Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Oocyte
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Epibatidine structure-activity relationships.
Carroll FI.
Bioorg Med Chem Lett (2004) 14 : 1889 -1896
PubMed 15050621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.02 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 7.85
CHEMBL301901 1 7.03
CHEMBL56682 1 6.59
CHEMBL56817 DESCHLOROEPIBATIDINE 1 5.44
CHEMBL56358 1 5.12
CHEMBL667 ACETYLCHOLINE 4.0 1 4.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE EC50 = 14.0 nM 7.85
CHEMBL301901 EC50 = 94.0 nM 7.03
CHEMBL56682 EC50 = 254.0 nM 6.59
CHEMBL56817 DESCHLOROEPIBATIDINE EC50 = 3630.0 nM 5.44
CHEMBL56358 EC50 = 7600.0 nM 5.12
CHEMBL667 ACETYLCHOLINE EC50 = 87000.0 nM 4.06