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Assay Detail

CHEMBL748208

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Binding
In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidinyl benzilate binding on rat brain stem homogenate.
ChEMBL ↗
48
Total Activities
44
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

Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
Moltzen EK, Pedersen H, Bøgesø KP, Meier E, Frederiksen K, Sánchez C, Løve Lembøl H.
J Med Chem (1994) 37 : 4085 -4099
PubMed 7990109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 6.92 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134063 — — 1 7.66
CHEMBL132894 — — 3 7.52
CHEMBL335308 — — 1 7.50
CHEMBL339438 — — 1 7.43
CHEMBL130693 — — 1 7.42
CHEMBL130689 — — 1 7.34
CHEMBL131095 — — 1 7.21
CHEMBL130111 — — 1 7.12
CHEMBL133961 — — 1 7.05
CHEMBL134177 — — 1 7.05
CHEMBL130688 — — 1 7.00
CHEMBL130842 — — 1 6.96
CHEMBL129998 — — 1 6.89
CHEMBL14 CARBACHOL 4.0 1 6.85
CHEMBL129886 — — 1 6.80
CHEMBL133905 — — 1 6.77
CHEMBL132503 — — 1 6.75
CHEMBL339175 — — 1 6.68
CHEMBL334493 — — 1 6.66
CHEMBL278422 — — 1 6.66
CHEMBL337474 — — 1 6.64
CHEMBL132502 — — 1 6.57
CHEMBL337676 — — 1 6.55
CHEMBL341193 — — 1 6.55
CHEMBL131777 — — 3 6.52
CHEMBL131428 ALVAMELINE 2.0 1 6.47
CHEMBL273308 — — 1 6.40
CHEMBL134122 — — 1 -
CHEMBL130342 — — 1 -
CHEMBL554487 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134063 — Ki = 22.0 nM 7.66
CHEMBL132894 — Ki = 30.0 nM 7.52
CHEMBL132894 — Ki = 30.0 nM 7.52
CHEMBL335308 — Ki = 32.0 nM 7.50
CHEMBL339438 — Ki = 37.0 nM 7.43
CHEMBL130693 — Ki = 38.0 nM 7.42
CHEMBL130689 — Ki = 46.0 nM 7.34
CHEMBL131095 — Ki = 61.0 nM 7.21
CHEMBL130111 — Ki = 75.0 nM 7.12
CHEMBL133961 — Ki = 90.0 nM 7.05
CHEMBL134177 — Ki = 90.0 nM 7.05
CHEMBL130688 — Ki = 100.0 nM 7.00
CHEMBL130842 — Ki = 110.0 nM 6.96
CHEMBL129998 — Ki = 130.0 nM 6.89
CHEMBL132894 — Ki = 130.0 nM 6.89
CHEMBL14 CARBACHOL Ki = 140.0 nM 6.85
CHEMBL129886 — Ki = 160.0 nM 6.80
CHEMBL133905 — Ki = 170.0 nM 6.77
CHEMBL132503 — Ki = 180.0 nM 6.75
CHEMBL339175 — Ki = 210.0 nM 6.68
CHEMBL334493 — Ki = 220.0 nM 6.66
CHEMBL278422 — Ki = 220.0 nM 6.66
CHEMBL337474 — Ki = 230.0 nM 6.64
CHEMBL132502 — Ki = 270.0 nM 6.57
CHEMBL341193 — Ki = 280.0 nM 6.55
CHEMBL337676 — Ki = 280.0 nM 6.55
CHEMBL131777 — Ki = 300.0 nM 6.52
CHEMBL131777 — Ki = 310.0 nM 6.51
CHEMBL131777 — Ki = 330.0 nM 6.48
CHEMBL131428 ALVAMELINE Ki = 340.0 nM 6.47
CHEMBL273308 — Ki = 400.0 nM 6.40
CHEMBL130148 — Ki - nM -
CHEMBL129923 — Ki - nM -
CHEMBL133986 — Ki - nM -
CHEMBL131753 — Ki - nM -
CHEMBL338122 — Ki - nM -
CHEMBL130387 — Ki - nM -
CHEMBL131249 — Ki - nM -
CHEMBL133184 — Ki - nM -
CHEMBL336834 — Ki - nM -
CHEMBL335920 — Ki - nM -
CHEMBL130625 — Ki - nM -
CHEMBL440903 — Ki - nM -
CHEMBL130127 — Ki - nM -
CHEMBL133680 — Ki - nM -
CHEMBL554487 — Ki - nM -
CHEMBL130342 — Ki - nM -
CHEMBL134122 — Ki - nM -