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Assay Detail

CHEMBL3618845

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Functional
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M4 (CHEMBL1821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M₁ agonists.
Liu B, Croy CH, Hitchcock SA, Allen JR, Rao Z, Evans D, Bures MG, McKinzie DL, Watt ML, Stuart Gregory G, Hansen MM, Hoogestraat PJ, Jamison JA, Okha-Mokube FM, Stratford RE, Turner W, Bymaster F, Felder CC.
Bioorg Med Chem Lett (2015) 25 : 4158 -4163
PubMed 26299349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.42 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL667 ACETYLCHOLINE 4.0 1 7.31
CHEMBL3616504 1 6.95
CHEMBL3618440 1 6.94
CHEMBL134641 SABCOMELINE 2.0 1 6.67
CHEMBL3618445 1 6.64
CHEMBL21536 XANOMELINE 4.0 1 6.64
CHEMBL3616499 1 6.63
CHEMBL3618444 1 6.45
CHEMBL3618449 1 6.41
CHEMBL3616500 1 6.41
CHEMBL3618450 1 6.39
CHEMBL2111051 TALSACLIDINE 2.0 1 6.07
CHEMBL3616501 1 5.97
CHEMBL3618436 1 5.96
CHEMBL3616497 1 5.87
CHEMBL3618447 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL667 ACETYLCHOLINE EC50 = 48.8 nM 7.31
CHEMBL3616504 EC50 = 113.0 nM 6.95
CHEMBL3618440 EC50 = 115.0 nM 6.94
CHEMBL134641 SABCOMELINE EC50 = 214.0 nM 6.67
CHEMBL3618445 EC50 = 227.0 nM 6.64
CHEMBL21536 XANOMELINE EC50 = 229.0 nM 6.64
CHEMBL3616499 EC50 = 235.0 nM 6.63
CHEMBL3618444 EC50 = 355.0 nM 6.45
CHEMBL3618449 EC50 = 392.0 nM 6.41
CHEMBL3616500 EC50 = 393.0 nM 6.41
CHEMBL3618450 EC50 = 405.0 nM 6.39
CHEMBL2111051 TALSACLIDINE EC50 = 844.0 nM 6.07
CHEMBL3616501 EC50 = 1060.0 nM 5.97
CHEMBL3618436 EC50 = 1110.0 nM 5.96
CHEMBL3616497 EC50 = 1360.0 nM 5.87
CHEMBL3618447 EC50 = 3720.0 nM 5.43