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Assay Detail

CHEMBL748902

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Binding
Binding affinity against muscarinic acetylcholine receptor M2 stably expressed in CHO-K1 cells using [3H]-QNB as radioligand.
35
Total Activities
35
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 Expert

Target

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

Publication

Sulfide analogues as potent and selective M(2) muscarinic receptor antagonists.
Wang Y, Chackalamannil S, Hu Z, McKittrick BA, Greenlee W, Ruperto V, Duffy RA, Lachowicz JE.
Bioorg Med Chem Lett (2002) 12 : 1087 -1091
PubMed 11909724 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.46 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11892 1 9.15
CHEMBL276239 1 9.05
CHEMBL12098 SCH-211803 1 9.05
CHEMBL11756 1 9.00
CHEMBL418530 1 8.57
CHEMBL12354 1 8.37
CHEMBL11527 1 8.21
CHEMBL12153 1 8.07
CHEMBL12542 1 7.96
CHEMBL11816 1 7.92
CHEMBL12064 1 7.85
CHEMBL12150 1 7.77
CHEMBL12085 1 7.75
CHEMBL11794 1 7.70
CHEMBL12228 1 7.70
CHEMBL440601 1 7.66
CHEMBL11893 1 7.66
CHEMBL275347 1 7.58
CHEMBL11690 1 7.40
CHEMBL12419 1 7.32
CHEMBL412421 1 6.98
CHEMBL12215 1 6.97
CHEMBL415975 1 6.89
CHEMBL12115 1 6.87
CHEMBL269645 1 6.87
CHEMBL11856 1 6.72
CHEMBL274999 1 6.62
CHEMBL273439 1 6.62
CHEMBL11877 1 6.60
CHEMBL12112 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11892 Ki = 0.7 nM 9.15
CHEMBL276239 Ki = 0.9 nM 9.05
CHEMBL12098 SCH-211803 Ki = 0.89 nM 9.05
CHEMBL11756 Ki = 1.0 nM 9.00
CHEMBL418530 Ki = 2.7 nM 8.57
CHEMBL12354 Ki = 4.3 nM 8.37
CHEMBL11527 Ki = 6.1 nM 8.21
CHEMBL12153 Ki = 8.6 nM 8.07
CHEMBL12542 Ki = 11.0 nM 7.96
CHEMBL11816 Ki = 12.0 nM 7.92
CHEMBL12064 Ki = 14.0 nM 7.85
CHEMBL12150 Ki = 17.0 nM 7.77
CHEMBL12085 Ki = 18.0 nM 7.75
CHEMBL11794 Ki = 20.0 nM 7.70
CHEMBL12228 Ki = 20.0 nM 7.70
CHEMBL440601 Ki = 22.0 nM 7.66
CHEMBL11893 Ki = 22.0 nM 7.66
CHEMBL275347 Ki = 26.0 nM 7.58
CHEMBL11690 Ki = 40.0 nM 7.40
CHEMBL12419 Ki = 48.0 nM 7.32
CHEMBL412421 Ki = 104.0 nM 6.98
CHEMBL12215 Ki = 108.0 nM 6.97
CHEMBL415975 Ki = 129.0 nM 6.89
CHEMBL12115 Ki = 134.0 nM 6.87
CHEMBL269645 Ki = 134.0 nM 6.87
CHEMBL11856 Ki = 192.0 nM 6.72
CHEMBL274999 Ki = 237.0 nM 6.62
CHEMBL273439 Ki = 241.0 nM 6.62
CHEMBL11877 Ki = 250.0 nM 6.60
CHEMBL12112 Ki = 256.0 nM 6.59
CHEMBL12268 Ki = 256.0 nM 6.59
CHEMBL12029 Ki = 254.0 nM 6.59
CHEMBL12291 Ki = 260.0 nM 6.58
CHEMBL11947 Ki = 923.0 nM 6.04
CHEMBL11710 Ki = 1500.0 nM 5.82