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Assay Detail

CHEMBL752414

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

Binding
Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors.
Böhme TM, Augelli-Szafran CE, Hallak H, Pugsley T, Serpa K, Schwarz RD.
J Med Chem (2002) 45 : 3094 -3102
PubMed 12086495 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.28 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106219 1 7.30
CHEMBL320465 1 7.15
CHEMBL106224 1 7.15
CHEMBL105148 1 7.04
CHEMBL104693 1 7.00
CHEMBL326450 1 6.82
CHEMBL106218 1 6.66
CHEMBL105122 1 6.64
CHEMBL280220 1 6.64
CHEMBL59898 1 6.59
CHEMBL107679 1 6.58
CHEMBL105160 1 6.55
CHEMBL318995 1 6.47
CHEMBL105945 1 6.40
CHEMBL420662 1 6.39
CHEMBL104210 1 6.34
CHEMBL104332 1 6.17
CHEMBL107444 1 6.04
CHEMBL106505 1 5.99
CHEMBL104574 1 5.86
CHEMBL104804 1 5.69
CHEMBL105674 1 5.56
CHEMBL104803 1 5.51
CHEMBL105593 1 5.29
CHEMBL106259 1 4.81
CHEMBL107680 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106219 Ki = 50.12 nM 7.30
CHEMBL320465 Ki = 70.79 nM 7.15
CHEMBL106224 Ki = 70.79 nM 7.15
CHEMBL105148 Ki = 91.2 nM 7.04
CHEMBL104693 Ki = 100.0 nM 7.00
CHEMBL326450 Ki = 151.36 nM 6.82
CHEMBL106218 Ki = 218.78 nM 6.66
CHEMBL105122 Ki = 229.09 nM 6.64
CHEMBL280220 Ki = 229.09 nM 6.64
CHEMBL59898 Ki = 257.04 nM 6.59
CHEMBL107679 Ki = 263.03 nM 6.58
CHEMBL105160 Ki = 281.84 nM 6.55
CHEMBL318995 Ki = 338.84 nM 6.47
CHEMBL105945 Ki = 398.11 nM 6.40
CHEMBL420662 Ki = 407.38 nM 6.39
CHEMBL104210 Ki = 457.09 nM 6.34
CHEMBL104332 Ki = 676.08 nM 6.17
CHEMBL107444 Ki = 912.01 nM 6.04
CHEMBL106505 Ki = 1023.29 nM 5.99
CHEMBL104574 Ki = 1380.38 nM 5.86
CHEMBL104804 Ki = 2041.74 nM 5.69
CHEMBL105674 Ki = 2754.23 nM 5.56
CHEMBL104803 Ki = 3090.3 nM 5.51
CHEMBL105593 Ki = 5128.61 nM 5.29
CHEMBL106259 Ki = 15488.17 nM 4.81
CHEMBL107680 Ki = 25703.96 nM 4.59