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Assay Detail

CHEMBL3424810

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

Binding
Displacement of [3H]epibatidine from rat alpha4beta2 nAChR transfected in HEK293 cells by liquid scintillation counting
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.
Beinat C, Reekie T, Banister SD, O'Brien-Brown J, Xie T, Olson TT, Xiao Y, Harvey A, O'Connor S, Coles C, Grishin A, Kolesik P, Tsanaktsidis J, Kassiou M.
Eur J Med Chem (2015) 95 : 277 -301
PubMed 25827398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 6.38 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1194009 1 6.38
CHEMBL3422595 1 -
CHEMBL3422575 1 -
CHEMBL3422574 1 -
CHEMBL1084615 1 -
CHEMBL3422572 1 -
CHEMBL3422571 1 -
CHEMBL3422570 1 -
CHEMBL3422569 1 -
CHEMBL3422568 1 -
CHEMBL568464 1 -
CHEMBL3422567 1 -
CHEMBL565963 1 -
CHEMBL3422573 1 -
CHEMBL3422597 1 -
CHEMBL3422596 1 -
CHEMBL3422594 1 -
CHEMBL3422593 1 -
CHEMBL3422592 1 -
CHEMBL3422591 1 -
CHEMBL3422590 1 -
CHEMBL3422582 1 -
CHEMBL1082655 1 -
CHEMBL3422588 1 -
CHEMBL3422587 1 -
CHEMBL3422586 1 -
CHEMBL3422585 1 -
CHEMBL3422584 1 -
CHEMBL3422583 1 -
CHEMBL3422589 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1194009 Ki = 417.0 nM 6.38
CHEMBL1084615 Ki > 10000.0 nM -
CHEMBL565963 Ki > 10000.0 nM -
CHEMBL3422567 Ki > 10000.0 nM -
CHEMBL568464 Ki - -
CHEMBL3422568 Ki - -
CHEMBL3422569 Ki > 10000.0 nM -
CHEMBL3422570 Ki > 10000.0 nM -
CHEMBL3422571 Ki > 10000.0 nM -
CHEMBL3422572 Ki > 10000.0 nM -
CHEMBL3422573 Ki > 10000.0 nM -
CHEMBL3422574 Ki > 10000.0 nM -
CHEMBL3422575 Ki > 10000.0 nM -
CHEMBL3422576 Ki > 10000.0 nM -
CHEMBL3422577 Ki > 10000.0 nM -
CHEMBL3422578 Ki > 10000.0 nM -
CHEMBL3422579 Ki > 10000.0 nM -
CHEMBL3422580 Ki > 10000.0 nM -
CHEMBL3422581 Ki > 10000.0 nM -
CHEMBL3422582 Ki > 10000.0 nM -
CHEMBL3422589 Ki > 10000.0 nM -
CHEMBL3422583 Ki > 10000.0 nM -
CHEMBL3422584 Ki > 10000.0 nM -
CHEMBL3422585 Ki > 50000.0 nM -
CHEMBL3422586 Ki > 10000.0 nM -
CHEMBL3422587 Ki > 100000.0 nM -
CHEMBL3422588 Ki > 10000.0 nM -
CHEMBL1082655 Ki > 30000.0 nM -
CHEMBL3422597 Ki > 10000.0 nM -
CHEMBL3422590 Ki - -
CHEMBL3422591 Ki > 10000.0 nM -
CHEMBL3422592 Ki > 10000.0 nM -
CHEMBL3422593 Ki > 10000.0 nM -
CHEMBL3422594 Ki > 10000.0 nM -
CHEMBL3422595 Ki > 10000.0 nM -
CHEMBL3422596 Ki > 10000.0 nM -