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Assay Detail

CHEMBL4815610

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

Binding
Displacement of [3H]-NMS from human muscarinic M2 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
ChEMBL ↗
79
Total Activities
79
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dibenzodiazepinone-type muscarinic receptor antagonists conjugated to basic peptides: Impact of the linker moiety and unnatural amino acids on M<sub>2</sub>R selectivity.
Weinhart CG, Wifling D, Schmidt MF, Neu E, Höring C, Clark T, Gmeiner P, Keller M.
Eur J Med Chem (2021) 213 : 113159 -113159
PubMed 33571911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 79 8.17 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4856113 — — 1 10.10
CHEMBL4597498 — — 1 10.00
CHEMBL4864727 — — 1 9.99
CHEMBL4859378 — — 1 9.98
CHEMBL4871700 — — 1 9.85
CHEMBL4861252 — — 1 9.82
CHEMBL4874955 — — 1 9.75
CHEMBL4852868 — — 1 9.73
CHEMBL4878646 — — 1 9.73
CHEMBL4851514 — — 1 9.72
CHEMBL4855492 — — 1 9.71
CHEMBL4448933 — — 1 9.70
CHEMBL4852186 — — 1 9.69
CHEMBL4862735 — — 1 9.68
CHEMBL4876725 — — 1 9.67
CHEMBL4876453 — — 1 9.67
CHEMBL4870127 — — 1 9.64
CHEMBL4864987 — — 1 9.62
CHEMBL4854886 — — 1 9.60
CHEMBL4863285 — — 1 9.59
CHEMBL4858398 — — 1 9.56
CHEMBL4871153 — — 1 9.54
CHEMBL4878717 — — 1 9.53
CHEMBL4847898 — — 1 9.51
CHEMBL295388 — — 1 9.50
CHEMBL4856659 — — 1 9.50
CHEMBL4862996 — — 1 9.48
CHEMBL4852646 — — 1 9.45
CHEMBL4872608 — — 1 9.42
CHEMBL4850130 — — 1 9.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4856113 — Ki = 0.07943 nM 10.10
CHEMBL4597498 — Ki = 0.1 nM 10.00
CHEMBL4864727 — Ki = 0.1023 nM 9.99
CHEMBL4859378 — Ki = 0.1047 nM 9.98
CHEMBL4871700 — Ki = 0.1413 nM 9.85
CHEMBL4861252 — Ki = 0.1514 nM 9.82
CHEMBL4874955 — Ki = 0.1778 nM 9.75
CHEMBL4852868 — Ki = 0.1862 nM 9.73
CHEMBL4878646 — Ki = 0.1862 nM 9.73
CHEMBL4851514 — Ki = 0.1905 nM 9.72
CHEMBL4855492 — Ki = 0.195 nM 9.71
CHEMBL4448933 — Ki = 0.1995 nM 9.70
CHEMBL4852186 — Ki = 0.2042 nM 9.69
CHEMBL4862735 — Ki = 0.2089 nM 9.68
CHEMBL4876453 — Ki = 0.2138 nM 9.67
CHEMBL4876725 — Ki = 0.2138 nM 9.67
CHEMBL4870127 — Ki = 0.2291 nM 9.64
CHEMBL4864987 — Ki = 0.2399 nM 9.62
CHEMBL4854886 — Ki = 0.2512 nM 9.60
CHEMBL4863285 — Ki = 0.257 nM 9.59
CHEMBL4858398 — Ki = 0.2754 nM 9.56
CHEMBL4871153 — Ki = 0.2884 nM 9.54
CHEMBL4878717 — Ki = 0.2951 nM 9.53
CHEMBL4847898 — Ki = 0.309 nM 9.51
CHEMBL4856659 — Ki = 0.3162 nM 9.50
CHEMBL295388 — Ki = 0.3162 nM 9.50
CHEMBL4862996 — Ki = 0.3311 nM 9.48
CHEMBL4852646 — Ki = 0.3548 nM 9.45
CHEMBL4872608 — Ki = 0.3802 nM 9.42
CHEMBL4850130 — Ki = 0.5888 nM 9.23
CHEMBL4059733 — Ki = 0.7943 nM 9.10
CHEMBL4865939 — Ki = 0.8318 nM 9.08
CHEMBL4862098 — Ki = 0.9333 nM 9.03
CHEMBL4596065 — Ki = 1.0 nM 9.00
CHEMBL4869723 — Ki = 1.175 nM 8.93
CHEMBL4846958 — Ki = 1.905 nM 8.72
CHEMBL4848683 — Ki = 2.291 nM 8.64
CHEMBL4857722 — Ki = 2.455 nM 8.61
CHEMBL4867301 — Ki = 2.951 nM 8.53
CHEMBL4862087 — Ki = 3.548 nM 8.45
CHEMBL4846562 — Ki = 7.244 nM 8.14
CHEMBL4872720 — Ki = 8.128 nM 8.09
CHEMBL4850553 — Ki = 12.02 nM 7.92
CHEMBL4873621 — Ki = 13.18 nM 7.88
CHEMBL4851265 — Ki = 14.79 nM 7.83
CHEMBL4867483 — Ki = 16.98 nM 7.77
CHEMBL4873979 — Ki = 17.78 nM 7.75
CHEMBL4861655 — Ki = 19.5 nM 7.71
CHEMBL4596899 — Ki = 19.95 nM 7.70
CHEMBL4863723 — Ki = 21.38 nM 7.67