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Assay Detail

CHEMBL863986

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

Binding
Binding affinity to human muscarinic M2 receptor
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.
Starck JP, Talaga P, Quéré L, Collart P, Christophe B, Lo Brutto P, Jadot S, Chimmanamada D, Zanda M, Wagner A, Mioskowski C, Massingham R, Guyaux M.
Bioorg Med Chem Lett (2006) 16 : 373 -377
PubMed 16275087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.74 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370232 1 9.70
CHEMBL200401 1 9.40
CHEMBL381623 1 9.10
CHEMBL200171 1 9.10
CHEMBL200319 1 8.89
CHEMBL203249 1 8.70
CHEMBL200693 1 8.70
CHEMBL382213 1 8.49
CHEMBL200432 1 8.49
CHEMBL1382 TOLTERODINE 4.0 1 8.40
CHEMBL427013 1 8.40
CHEMBL383389 1 8.30
CHEMBL201933 1 8.30
CHEMBL200957 1 7.89
CHEMBL1231 OXYBUTYNIN 4.0 1 7.80
CHEMBL371734 1 7.70
CHEMBL381878 1 7.70
CHEMBL200416 1 7.60
CHEMBL199821 1 7.40
CHEMBL383248 1 7.40
CHEMBL1346 DARIFENACIN 4.0 1 7.30
CHEMBL380583 1 7.30
CHEMBL370862 1 7.30
CHEMBL372566 1 7.30
CHEMBL200210 1 7.10
CHEMBL381469 1 7.00
CHEMBL199981 1 6.90
CHEMBL373256 1 6.60
CHEMBL200208 1 6.60
CHEMBL381020 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370232 Ki = 0.2 nM 9.70
CHEMBL200401 Ki = 0.4 nM 9.40
CHEMBL381623 Ki = 0.79 nM 9.10
CHEMBL200171 Ki = 0.79 nM 9.10
CHEMBL200319 Ki = 1.3 nM 8.89
CHEMBL203249 Ki = 2.0 nM 8.70
CHEMBL200693 Ki = 2.0 nM 8.70
CHEMBL382213 Ki = 3.2 nM 8.49
CHEMBL200432 Ki = 3.2 nM 8.49
CHEMBL1382 TOLTERODINE Ki = 4.0 nM 8.40
CHEMBL427013 Ki = 4.0 nM 8.40
CHEMBL383389 Ki = 5.0 nM 8.30
CHEMBL201933 Ki = 5.0 nM 8.30
CHEMBL200957 Ki = 13.0 nM 7.89
CHEMBL1231 OXYBUTYNIN Ki = 16.0 nM 7.80
CHEMBL381878 Ki = 20.0 nM 7.70
CHEMBL371734 Ki = 20.0 nM 7.70
CHEMBL200416 Ki = 25.0 nM 7.60
CHEMBL199821 Ki = 40.0 nM 7.40
CHEMBL383248 Ki = 40.0 nM 7.40
CHEMBL1346 DARIFENACIN Ki = 50.0 nM 7.30
CHEMBL380583 Ki = 50.0 nM 7.30
CHEMBL370862 Ki = 50.0 nM 7.30
CHEMBL372566 Ki = 50.0 nM 7.30
CHEMBL200210 Ki = 79.0 nM 7.10
CHEMBL381469 Ki = 100.0 nM 7.00
CHEMBL199981 Ki = 126.0 nM 6.90
CHEMBL373256 Ki = 251.0 nM 6.60
CHEMBL200208 Ki = 251.0 nM 6.60
CHEMBL381020 Ki = 316.0 nM 6.50
CHEMBL200209 Ki = 501.0 nM 6.30
CHEMBL200566 Ki = 631.0 nM 6.20
CHEMBL197973 Ki = 3161.0 nM 5.50