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Assay Detail

CHEMBL4605252

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

ADMET
Displacement of [3H]-QNB from Wistar rat heart muscarinic M2 receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M2 (CHEMBL309)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.
Fischer O, Hofmann J, Rampp H, Kaindl J, Pratsch G, Bartuschat A, Taudte RV, Fromm MF, Hübner H, Gmeiner P, Heinrich MR.
J Med Chem (2020) 63 : 4349 -4369
PubMed 32202101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.35 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644670 1 8.12
CHEMBL1683908 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644670 Ki = 7.6 nM 8.12
CHEMBL1683908 Ki = 270.0 nM 6.57