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Assay Detail

CHEMBL745740

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

Binding
Binding affinity against M1 receptor expressed in CHO-K1 cells transfected with human muscarinic receptor sequence using radioligand [3H]quinuclidinyl benzilate ([3H]QNB)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity
Malaska MJ, Fauq AH, Kozikowski AP, Aagaard PJ, McKinney M
Bioorg Med Chem Lett (1995) 5 : 61 -66
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.31 6.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277642 HIMBACINE 1 6.83
CHEMBL160666 1 6.78
CHEMBL159237 1 6.37
CHEMBL346049 1 6.31
CHEMBL159189 1 6.22
CHEMBL160755 1 6.06
CHEMBL158589 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277642 HIMBACINE Kd = 148.0 nM 6.83
CHEMBL160666 Kd = 167.0 nM 6.78
CHEMBL159237 Kd = 423.0 nM 6.37
CHEMBL346049 Kd = 494.0 nM 6.31
CHEMBL159189 Kd = 604.7 nM 6.22
CHEMBL160755 Kd = 866.0 nM 6.06
CHEMBL158589 Kd = 2520.0 nM 5.60