Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2380035

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

Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M1 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.
Bhattacharjee AK, Pomponio JW, Evans SA, Pervitsky D, Gordon RK.
Bioorg Med Chem (2013) 21 : 2651 -2662
PubMed 23523385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.81 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2377266 1 9.23
CHEMBL37372 1 9.05
CHEMBL517712 ATROPINE 4.0 1 9.04
CHEMBL2377387 1 8.89
CHEMBL2377267 1 8.88
CHEMBL2106570 METHYLBENACTYZIUM BROMIDE 2.0 1 8.80
CHEMBL1101 BIPERIDEN 4.0 1 8.63
CHEMBL2377385 1 8.24
CHEMBL2377383 1 8.24
CHEMBL2377269 1 8.11
CHEMBL2377392 1 7.97
CHEMBL26505 APROFENE 2.0 1 7.82
CHEMBL2377384 1 7.07
CHEMBL1191560 1 6.78
CHEMBL2377388 1 6.75
CHEMBL2110892 BIETAMIVERINE 2.0 1 6.57
CHEMBL2377262 1 6.29
CHEMBL2377261 1 6.01
CHEMBL2377264 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2377266 Ki = 0.594 nM 9.23
CHEMBL37372 Ki = 0.881 nM 9.05
CHEMBL517712 ATROPINE Ki = 0.922 nM 9.04
CHEMBL2377387 Ki = 1.29 nM 8.89
CHEMBL2377267 Ki = 1.32 nM 8.88
CHEMBL2106570 METHYLBENACTYZIUM BROMIDE Ki = 1.59 nM 8.80
CHEMBL1101 BIPERIDEN Ki = 2.36 nM 8.63
CHEMBL2377385 Ki = 5.78 nM 8.24
CHEMBL2377383 Ki = 5.75 nM 8.24
CHEMBL2377269 Ki = 7.75 nM 8.11
CHEMBL2377392 Ki = 10.7 nM 7.97
CHEMBL26505 APROFENE Ki = 15.1 nM 7.82
CHEMBL2377384 Ki = 85.7 nM 7.07
CHEMBL1191560 Ki = 166.0 nM 6.78
CHEMBL2377388 Ki = 176.0 nM 6.75
CHEMBL2110892 BIETAMIVERINE Ki = 271.0 nM 6.57
CHEMBL2377262 Ki = 519.0 nM 6.29
CHEMBL2377261 Ki = 971.0 nM 6.01
CHEMBL2377264 Ki = 1040.0 nM 5.98