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Assay Detail

CHEMBL744248

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

Binding
Inhibition of specific binding of [3H]NMS to Muscarinic acetylcholine receptor in rat cerebral cortex by using competitive binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
Lundkvist JR, Vargas HM, Caldirola P, Ringdahl B, Hacksell U.
J Med Chem (1990) 33 : 3182 -3189
PubMed 2258904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.20 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2092930 1 7.80
CHEMBL1788225 1 7.38
CHEMBL107456 1 7.36
CHEMBL1788202 1 7.19
CHEMBL432629 1 7.09
CHEMBL1788224 1 6.39
CHEMBL110892 1 6.17
CHEMBL108140 1 6.12
CHEMBL106056 1 5.91
CHEMBL1788219 1 5.83
CHEMBL2092931 1 5.68
CHEMBL108582 1 5.65
CHEMBL108557 1 5.54
CHEMBL322126 1 5.29
CHEMBL111327 1 5.21
CHEMBL323032 1 4.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2092930 Ki = 16.0 nM 7.80
CHEMBL1788225 Ki = 42.0 nM 7.38
CHEMBL107456 Ki = 44.0 nM 7.36
CHEMBL1788202 Ki = 64.0 nM 7.19
CHEMBL432629 Ki = 82.0 nM 7.09
CHEMBL1788224 Ki = 410.0 nM 6.39
CHEMBL110892 Ki = 670.0 nM 6.17
CHEMBL108140 Ki = 750.0 nM 6.12
CHEMBL106056 Ki = 1230.0 nM 5.91
CHEMBL1788219 Ki = 1482.0 nM 5.83
CHEMBL2092931 Ki = 2070.0 nM 5.68
CHEMBL108582 Ki = 2260.0 nM 5.65
CHEMBL108557 Ki = 2900.0 nM 5.54
CHEMBL322126 Ki = 5160.0 nM 5.29
CHEMBL111327 Ki = 6100.0 nM 5.21
CHEMBL323032 Ki = 25400.0 nM 4.59