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Assay Detail

CHEMBL863985

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

Binding
Binding affinity to human muscarinic M3 receptor
34
Total Activities
34
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 M3 (CHEMBL245)
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 34 8.50 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370232 1 10.30
CHEMBL200401 1 10.10
CHEMBL381623 1 9.89
CHEMBL200693 1 9.70
CHEMBL200432 1 9.60
CHEMBL200171 1 9.60
CHEMBL427013 1 9.49
CHEMBL200319 1 9.40
CHEMBL200416 1 9.20
CHEMBL382213 1 9.10
CHEMBL383389 1 9.10
CHEMBL203249 1 9.00
CHEMBL200957 1 9.00
CHEMBL381878 1 9.00
CHEMBL1231 OXYBUTYNIN 4.0 1 8.89
CHEMBL201933 1 8.89
CHEMBL1346 DARIFENACIN 4.0 1 8.89
CHEMBL199821 1 8.60
CHEMBL371734 1 8.49
CHEMBL1382 TOLTERODINE 4.0 1 8.49
CHEMBL370862 1 8.40
CHEMBL380583 1 8.10
CHEMBL199981 1 8.10
CHEMBL383248 1 8.10
CHEMBL200210 1 8.00
CHEMBL372566 1 7.89
CHEMBL381020 1 7.70
CHEMBL373256 1 7.40
CHEMBL381469 1 7.30
CHEMBL200208 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370232 Ki = 0.05 nM 10.30
CHEMBL200401 Ki = 0.08 nM 10.10
CHEMBL381623 Ki = 0.13 nM 9.89
CHEMBL200693 Ki = 0.2 nM 9.70
CHEMBL200432 Ki = 0.25 nM 9.60
CHEMBL200171 Ki = 0.25 nM 9.60
CHEMBL427013 Ki = 0.32 nM 9.49
CHEMBL200319 Ki = 0.4 nM 9.40
CHEMBL200416 Ki = 0.63 nM 9.20
CHEMBL382213 Ki = 0.79 nM 9.10
CHEMBL383389 Ki = 0.79 nM 9.10
CHEMBL203249 Ki = 1.0 nM 9.00
CHEMBL200957 Ki = 1.0 nM 9.00
CHEMBL381878 Ki = 1.0 nM 9.00
CHEMBL1346 DARIFENACIN Ki = 1.3 nM 8.89
CHEMBL1231 OXYBUTYNIN Ki = 1.3 nM 8.89
CHEMBL201933 Ki = 1.3 nM 8.89
CHEMBL199821 Ki = 2.5 nM 8.60
CHEMBL371734 Ki = 3.2 nM 8.49
CHEMBL1382 TOLTERODINE Ki = 3.2 nM 8.49
CHEMBL370862 Ki = 4.0 nM 8.40
CHEMBL380583 Ki = 7.9 nM 8.10
CHEMBL199981 Ki = 7.9 nM 8.10
CHEMBL383248 Ki = 7.9 nM 8.10
CHEMBL200210 Ki = 10.0 nM 8.00
CHEMBL372566 Ki = 13.0 nM 7.89
CHEMBL381020 Ki = 20.0 nM 7.70
CHEMBL373256 Ki = 40.0 nM 7.40
CHEMBL381469 Ki = 50.0 nM 7.30
CHEMBL200208 Ki = 63.0 nM 7.20
CHEMBL200209 Ki = 100.0 nM 7.00
CHEMBL200566 Ki = 100.0 nM 7.00
CHEMBL197973 Ki = 631.0 nM 6.20
CHEMBL199591 Ki = 1000.0 nM 6.00