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Assay Detail

CHEMBL744915

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Binding
In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidinyl benzilate binding on rat brain homogenate
ChEMBL ↗
49
Total Activities
45
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 49 6.65 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130111 — — 1 7.42
CHEMBL134063 — — 1 7.39
CHEMBL335308 — — 1 7.37
CHEMBL130693 — — 1 7.33
CHEMBL339438 — — 1 7.32
CHEMBL334493 — — 1 7.09
CHEMBL132503 — — 1 7.00
CHEMBL278422 — — 1 7.00
CHEMBL131095 — — 1 6.96
CHEMBL130842 — — 1 6.89
CHEMBL130689 — — 1 6.85
CHEMBL130927 — — 1 6.85
CHEMBL131777 — — 3 6.72
CHEMBL134177 — — 1 6.64
CHEMBL132894 — — 3 6.64
CHEMBL130688 — — 1 6.64
CHEMBL129998 — — 1 6.60
CHEMBL339175 — — 1 6.57
CHEMBL129886 — — 1 6.55
CHEMBL133905 — — 1 6.54
CHEMBL131428 ALVAMELINE 2.0 1 6.37
CHEMBL341193 — — 1 6.28
CHEMBL132502 — — 1 6.28
CHEMBL133961 — — 1 6.24
CHEMBL273308 — — 1 6.16
CHEMBL337474 — — 1 6.10
CHEMBL14 CARBACHOL 4.0 1 5.96
CHEMBL337676 — — 1 5.80
CHEMBL336834 — — 1 -
CHEMBL133680 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130111 — Ki = 38.0 nM 7.42
CHEMBL134063 — Ki = 41.0 nM 7.39
CHEMBL335308 — Ki = 43.0 nM 7.37
CHEMBL130693 — Ki = 47.0 nM 7.33
CHEMBL339438 — Ki = 48.0 nM 7.32
CHEMBL334493 — Ki = 81.0 nM 7.09
CHEMBL278422 — Ki = 100.0 nM 7.00
CHEMBL132503 — Ki = 100.0 nM 7.00
CHEMBL131095 — Ki = 110.0 nM 6.96
CHEMBL130842 — Ki = 130.0 nM 6.89
CHEMBL130689 — Ki = 140.0 nM 6.85
CHEMBL130927 — Ki = 140.0 nM 6.85
CHEMBL131777 — Ki = 190.0 nM 6.72
CHEMBL134177 — Ki = 230.0 nM 6.64
CHEMBL132894 — Ki = 230.0 nM 6.64
CHEMBL130688 — Ki = 230.0 nM 6.64
CHEMBL129998 — Ki = 250.0 nM 6.60
CHEMBL132894 — Ki = 270.0 nM 6.57
CHEMBL339175 — Ki = 270.0 nM 6.57
CHEMBL129886 — Ki = 280.0 nM 6.55
CHEMBL133905 — Ki = 290.0 nM 6.54
CHEMBL132894 — Ki = 320.0 nM 6.50
CHEMBL131428 ALVAMELINE Ki = 430.0 nM 6.37
CHEMBL131777 — Ki = 530.0 nM 6.28
CHEMBL132502 — Ki = 530.0 nM 6.28
CHEMBL341193 — Ki = 530.0 nM 6.28
CHEMBL133961 — Ki = 570.0 nM 6.24
CHEMBL273308 — Ki = 690.0 nM 6.16
CHEMBL337474 — Ki = 790.0 nM 6.10
CHEMBL131777 — Ki = 910.0 nM 6.04
CHEMBL14 CARBACHOL Ki = 1100.0 nM 5.96
CHEMBL337676 — Ki = 1600.0 nM 5.80
CHEMBL130387 — Ki - nM -
CHEMBL130625 — Ki - nM -
CHEMBL133184 — Ki - nM -
CHEMBL338122 — Ki - nM -
CHEMBL131753 — Ki - nM -
CHEMBL133986 — Ki - nM -
CHEMBL129923 — Ki - nM -
CHEMBL336834 — Ki - nM -
CHEMBL131249 — Ki - nM -
CHEMBL554487 — Ki - nM -
CHEMBL130342 — Ki - nM -
CHEMBL130127 — Ki - nM -
CHEMBL134122 — Ki - nM -
CHEMBL335920 — Ki - nM -
CHEMBL440903 — Ki - nM -
CHEMBL133680 — Ki - nM -
CHEMBL130148 — Ki - nM -