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Assay Detail

CHEMBL752311

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

Binding
Inhibition of [3H]QNB binding against muscarinic acetylcholine receptor in rat brain.
22
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.
Triggle DJ, Kwon YW, Abraham P, Pitner JB, Mascarella SW, Carroll FI.
J Med Chem (1991) 34 : 3164 -3171
PubMed 1956033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.94 10.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320611 3 10.53
CHEMBL321214 1 9.65
CHEMBL318812 1 9.60
CHEMBL517712 ATROPINE 4.0 1 9.47
CHEMBL326640 1 8.72
CHEMBL110808 1 8.39
CHEMBL110339 1 8.38
CHEMBL322582 1 8.02
CHEMBL550 PILOCARPINE 4.0 1 6.00
CHEMBL326453 1 5.45
CHEMBL111529 3 5.43
CHEMBL2113669 2 5.33
CHEMBL325322 3 5.19
CHEMBL607175 1 5.00
CHEMBL14 CARBACHOL 4.0 1 4.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320611 Ki = 0.0297 nM 10.53
CHEMBL320611 Ki = 0.13 nM 9.89
CHEMBL321214 Ki = 0.224 nM 9.65
CHEMBL318812 Ki = 0.254 nM 9.60
CHEMBL517712 ATROPINE Ki = 0.337 nM 9.47
CHEMBL326640 Ki = 1.89 nM 8.72
CHEMBL110808 Ki = 4.07 nM 8.39
CHEMBL110339 Ki = 4.2 nM 8.38
CHEMBL320611 Ki = 6.36 nM 8.20
CHEMBL322582 Ki = 9.53 nM 8.02
CHEMBL550 PILOCARPINE Ki = 1010.0 nM 6.00
CHEMBL326453 Ki = 3530.0 nM 5.45
CHEMBL111529 Ki = 3730.0 nM 5.43
CHEMBL2113669 Ki = 4710.0 nM 5.33
CHEMBL325322 Ki = 6470.0 nM 5.19
CHEMBL111529 Ki = 7530.0 nM 5.12
CHEMBL111529 Ki = 8560.0 nM 5.07
CHEMBL325322 Ki = 8550.0 nM 5.07
CHEMBL607175 Ki = 10100.0 nM 5.00
CHEMBL14 CARBACHOL Ki = 18800.0 nM 4.73
CHEMBL2113669 Ki = 19100.0 nM 4.72
CHEMBL325322 Ki = 23000.0 nM 4.64