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Assay Detail

CHEMBL3618843

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

Functional
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
23
Total Activities
23
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 M3 (CHEMBL245)
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 23 6.40 6.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134641 SABCOMELINE 2.0 1 6.93
CHEMBL667 ACETYLCHOLINE 4.0 1 6.69
CHEMBL2111051 TALSACLIDINE 2.0 1 5.57
CHEMBL3618437 1 -
CHEMBL3618438 1 -
CHEMBL3618439 1 -
CHEMBL3618440 1 -
CHEMBL3618441 1 -
CHEMBL3618442 1 -
CHEMBL3618443 1 -
CHEMBL3618444 1 -
CHEMBL3618445 1 -
CHEMBL3618446 1 -
CHEMBL3618436 1 -
CHEMBL3618447 1 -
CHEMBL3618448 1 -
CHEMBL3618449 1 -
CHEMBL3618450 1 -
CHEMBL3616498 1 -
CHEMBL3616499 1 -
CHEMBL3616500 1 -
CHEMBL3616501 1 -
CHEMBL3616497 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134641 SABCOMELINE EC50 = 117.0 nM 6.93
CHEMBL667 ACETYLCHOLINE EC50 = 205.0 nM 6.69
CHEMBL2111051 TALSACLIDINE EC50 = 2696.0 nM 5.57
CHEMBL3618437 EC50 - -
CHEMBL3618438 EC50 - -
CHEMBL3618439 EC50 - -
CHEMBL3618440 EC50 - -
CHEMBL3618441 EC50 - -
CHEMBL3618442 EC50 - -
CHEMBL3618443 EC50 - -
CHEMBL3618444 EC50 - -
CHEMBL3618445 EC50 - -
CHEMBL3618446 EC50 - -
CHEMBL3618436 EC50 - -
CHEMBL3618447 EC50 - -
CHEMBL3618448 EC50 - -
CHEMBL3618449 EC50 - -
CHEMBL3618450 EC50 - -
CHEMBL3616498 EC50 - -
CHEMBL3616499 EC50 - -
CHEMBL3616500 EC50 - -
CHEMBL3616501 EC50 - -
CHEMBL3616497 EC50 - -