Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL745634

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

Functional
Stimulation of cAMP in CHO cells expressing human m2 receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.
Sauerberg P, Jeppesen L, Olesen PH, Sheardown MJ, Fink-Jensen A, Rasmussen T, Rimvall K, Shannon HE, Bymaster FP, DeLapp NW, Calligaro DO, Ward JS, Whitesitt CA, Thomsen C.
Bioorg Med Chem Lett (1998) 8 : 2897 -2902
PubMed 9873644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 6.45 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL100147 1 8.70
CHEMBL98255 1 8.05
CHEMBL327269 1 7.96
CHEMBL4524086 1 7.54
CHEMBL99521 1 7.21
CHEMBL99884 1 6.86
CHEMBL319109 1 6.64
CHEMBL291351 1 6.62
CHEMBL14 CARBACHOL 4.0 1 6.16
CHEMBL60419 1 6.11
CHEMBL1169506 1 5.97
CHEMBL100163 1 5.96
CHEMBL4524085 1 5.65
CHEMBL7303 ARECOLINE -1.0 1 5.00
CHEMBL81878 1 4.55
CHEMBL550 PILOCARPINE 4.0 1 4.20
CHEMBL316625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL100147 EC50 = 2.0 nM 8.70
CHEMBL98255 EC50 = 9.0 nM 8.05
CHEMBL327269 EC50 = 11.0 nM 7.96
CHEMBL4524086 EC50 = 29.0 nM 7.54
CHEMBL99521 EC50 = 62.0 nM 7.21
CHEMBL99884 EC50 = 139.0 nM 6.86
CHEMBL319109 EC50 = 227.0 nM 6.64
CHEMBL291351 EC50 = 240.0 nM 6.62
CHEMBL14 CARBACHOL EC50 = 700.0 nM 6.16
CHEMBL60419 EC50 = 779.0 nM 6.11
CHEMBL1169506 EC50 = 1075.0 nM 5.97
CHEMBL100163 EC50 = 1096.0 nM 5.96
CHEMBL4524085 EC50 = 2253.0 nM 5.65
CHEMBL7303 ARECOLINE EC50 = 10000.0 nM 5.00
CHEMBL81878 EC50 = 28000.0 nM 4.55
CHEMBL550 PILOCARPINE EC50 = 63000.0 nM 4.20
CHEMBL316625 EC50 > 10000.0 nM -