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Assay Detail

CHEMBL828817

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

Binding
Affinity for rat Muscarinic acetylcholine receptor M3
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M3 (CHEMBL320)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis and activity of novel derivatives of oxybutynin and tolterodine.
Kaur K, Aeron S, Bruhaspathy M, Shetty SJ, Gupta S, Hegde LH, Silamkoti AD, Mehta A, Chugh A, Gupta JB, Sarma PK, Kumar N.
Bioorg Med Chem Lett (2005) 15 : 2093 -2096
PubMed 15808475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.15 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1231 OXYBUTYNIN 4.0 1 9.02
CHEMBL1382 TOLTERODINE 4.0 1 8.15
CHEMBL192065 1 7.85
CHEMBL192061 2 7.60
CHEMBL192537 1 7.46
CHEMBL192485 2 7.43
CHEMBL192337 1 7.41
CHEMBL190815 1 7.30
CHEMBL192885 1 6.93
CHEMBL195169 1 6.54
CHEMBL194870 1 6.44
CHEMBL190459 1 6.02
CHEMBL424832 1 5.58
CHEMBL372462 1 -
CHEMBL363865 1 -
CHEMBL370757 1 -
CHEMBL192083 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1231 OXYBUTYNIN Ki = 0.95 nM 9.02
CHEMBL1382 TOLTERODINE Ki = 7.07 nM 8.15
CHEMBL192065 Ki = 14.0 nM 7.85
CHEMBL192061 Ki = 25.0 nM 7.60
CHEMBL192537 Ki = 35.0 nM 7.46
CHEMBL192485 Ki = 37.0 nM 7.43
CHEMBL192337 Ki = 39.0 nM 7.41
CHEMBL190815 Ki = 50.0 nM 7.30
CHEMBL192061 Ki = 79.0 nM 7.10
CHEMBL192885 Ki = 118.0 nM 6.93
CHEMBL195169 Ki = 291.0 nM 6.54
CHEMBL192485 Ki = 330.0 nM 6.48
CHEMBL194870 Ki = 366.0 nM 6.44
CHEMBL190459 Ki = 964.0 nM 6.02
CHEMBL424832 Ki = 2605.0 nM 5.58
CHEMBL372462 Ki > 1000.0 nM -
CHEMBL363865 Ki > 1000.0 nM -
CHEMBL370757 Ki > 1000.0 nM -
CHEMBL192083 Ki > 10000.0 nM -