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Assay Detail

CHEMBL750087

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

Binding
Binding affinity towards rat alpha2-beta2 neuronal nAChR expressed in Xenopus oocytes using [3H]epibatidine as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuronal acetylcholine receptor; alpha2/beta2 (CHEMBL1907592)
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
Ki 8 10.66 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 11.00
CHEMBL301901 1 10.89
CHEMBL56817 DESCHLOROEPIBATIDINE 1 10.55
CHEMBL56358 1 10.21
CHEMBL56682 1 -
CHEMBL54585 1 -
CHEMBL300837 1 -
CHEMBL56677 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.01 nM 11.00
CHEMBL301901 Ki = 0.013 nM 10.89
CHEMBL56817 DESCHLOROEPIBATIDINE Ki = 0.028 nM 10.55
CHEMBL56358 Ki = 0.062 nM 10.21
CHEMBL56682 Ki = 0.0024 nM -
CHEMBL54585 Ki > 100.0 nM -
CHEMBL300837 Ki > 10.0 nM -
CHEMBL56677 Ki > 100.0 nM -