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Assay Detail

CHEMBL751550

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

Binding
Binding activity to the muscarinic acetylcholine receptor in rat cortex, assayed using [3H]PZ as a radioligand.
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Chemical and biochemical studies of 2-propynylpyrrolidine derivatives. Restricted-rotation analogues of N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide (BM-5).
Trybulski EJ, Kramss RH, Mangano RM, Rusinko A.
J Med Chem (1990) 33 : 3190 -3198
PubMed 2258905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 5.80 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310852 1 7.40
CHEMBL108439 1 7.16
CHEMBL107491 1 7.00
CHEMBL2092935 1 6.85
CHEMBL7634 OXOTREMORINE 1 6.85
CHEMBL2092936 1 6.77
CHEMBL2111700 1 6.72
CHEMBL326905 1 6.38
CHEMBL2111699 1 5.93
CHEMBL110208 1 5.91
CHEMBL111087 1 5.83
CHEMBL2111696 1 5.80
CHEMBL2111697 1 5.79
CHEMBL1203011 1 5.69
CHEMBL1203014 1 5.65
CHEMBL1203010 1 5.51
CHEMBL2092934 1 5.39
CHEMBL2111698 1 5.28
CHEMBL2111695 1 5.25
CHEMBL14 CARBACHOL 4.0 1 5.24
CHEMBL1203012 1 5.22
CHEMBL2092938 1 5.19
CHEMBL107713 1 5.04
CHEMBL1203013 1 4.88
CHEMBL321684 1 4.86
CHEMBL2092937 1 4.60
CHEMBL108411 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310852 Ki = 40.0 nM 7.40
CHEMBL108439 Ki = 70.0 nM 7.16
CHEMBL107491 Ki = 100.0 nM 7.00
CHEMBL2092935 Ki = 140.0 nM 6.85
CHEMBL7634 OXOTREMORINE Ki = 140.0 nM 6.85
CHEMBL2092936 Ki = 170.0 nM 6.77
CHEMBL2111700 Ki = 190.0 nM 6.72
CHEMBL326905 Ki = 420.0 nM 6.38
CHEMBL2111699 Ki = 1180.0 nM 5.93
CHEMBL110208 Ki = 1230.0 nM 5.91
CHEMBL111087 Ki = 1480.0 nM 5.83
CHEMBL2111696 Ki = 1590.0 nM 5.80
CHEMBL2111697 Ki = 1630.0 nM 5.79
CHEMBL1203011 Ki = 2060.0 nM 5.69
CHEMBL1203014 Ki = 2220.0 nM 5.65
CHEMBL1203010 Ki = 3100.0 nM 5.51
CHEMBL2092934 Ki = 4110.0 nM 5.39
CHEMBL2111698 Ki = 5250.0 nM 5.28
CHEMBL2111695 Ki = 5600.0 nM 5.25
CHEMBL14 CARBACHOL Ki = 5800.0 nM 5.24
CHEMBL1203012 Ki = 6050.0 nM 5.22
CHEMBL2092938 Ki = 6500.0 nM 5.19
CHEMBL107713 Ki = 9040.0 nM 5.04
CHEMBL1203013 Ki = 13200.0 nM 4.88
CHEMBL321684 Ki = 13900.0 nM 4.86
CHEMBL2092937 Ki = 25200.0 nM 4.60
CHEMBL108411 Ki = 40000.0 nM 4.40