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Assay Detail

CHEMBL938553

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Functional
Agonist activity at muscarinic M1 receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
Miller NR, Daniels RN, Bridges TM, Brady AE, Conn PJ, Lindsley CW.
Bioorg Med Chem Lett (2008) 18 : 5443 -5447
PubMed 18829311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 5.67 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522460 1 6.54
CHEMBL478662 1 6.48
CHEMBL513765 1 6.29
CHEMBL471213 1 6.06
CHEMBL511833 1 6.04
CHEMBL487557 1 6.03
CHEMBL487762 1 5.85
CHEMBL471636 1 5.68
CHEMBL485913 1 5.68
CHEMBL485755 1 5.64
CHEMBL486758 1 5.58
CHEMBL471635 1 5.57
CHEMBL485953 1 5.48
CHEMBL487986 1 5.44
CHEMBL521030 1 5.39
CHEMBL487984 1 5.36
CHEMBL486331 1 5.19
CHEMBL487558 1 5.15
CHEMBL487985 1 5.02
CHEMBL521388 1 4.96
CHEMBL487788 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522460 EC50 = 289.0 nM 6.54
CHEMBL478662 EC50 = 334.0 nM 6.48
CHEMBL513765 EC50 = 510.0 nM 6.29
CHEMBL471213 EC50 = 880.0 nM 6.06
CHEMBL511833 EC50 = 910.0 nM 6.04
CHEMBL487557 EC50 = 930.0 nM 6.03
CHEMBL487762 EC50 = 1400.0 nM 5.85
CHEMBL471636 EC50 = 2110.0 nM 5.68
CHEMBL485913 EC50 = 2100.0 nM 5.68
CHEMBL485755 EC50 = 2300.0 nM 5.64
CHEMBL486758 EC50 = 2600.0 nM 5.58
CHEMBL471635 EC50 = 2710.0 nM 5.57
CHEMBL485953 EC50 = 3300.0 nM 5.48
CHEMBL487986 EC50 = 3600.0 nM 5.44
CHEMBL521030 EC50 = 4100.0 nM 5.39
CHEMBL487984 EC50 = 4400.0 nM 5.36
CHEMBL486331 EC50 = 6500.0 nM 5.19
CHEMBL487558 EC50 = 7110.0 nM 5.15
CHEMBL487985 EC50 = 9600.0 nM 5.02
CHEMBL521388 EC50 = 11100.0 nM 4.96
CHEMBL487788 EC50 > 10000.0 nM -