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Assay Detail

CHEMBL3620132

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

Binding
Displacement of [3H]epibatidine from rat alpha3beta4 nACHR expressed in HEK293 cells after 4 hrs by scintillation counting assay
ChEMBL ↗
66
Total Activities
33
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; alpha3/beta4 (CHEMBL1907593) ↗
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Exploration of the molecular architecture of the orthosteric binding site in the α4β2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.
Bach TB, Jensen AA, Petersen JG, Sørensen TE, Della Volpe S, Liu J, Blaazer AR, van Muijlwijk-Koezen JE, Balle T, Frølund B.
Eur J Med Chem (2015) 102 : 425 -444
PubMed 26301559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 66 5.13 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122270 LOBELINE 2.0 2 6.32
CHEMBL667 ACETYLCHOLINE 4.0 2 6.21
CHEMBL3616578 — — 2 6.11
CHEMBL3616573 — — 2 5.66
CHEMBL3616575 — — 2 5.59
CHEMBL3616574 — — 2 5.54
CHEMBL3616576 — — 2 5.47
CHEMBL3616577 — — 2 5.42
CHEMBL3616562 — — 2 5.23
CHEMBL3616561 — — 2 5.16
CHEMBL1090908 — — 2 5.09
CHEMBL3616572 — — 2 5.08
CHEMBL466400 — — 2 5.00
CHEMBL3616560 — — 2 4.97
CHEMBL3616559 — — 2 4.89
CHEMBL1090909 — — 2 4.70
CHEMBL3616570 — — 2 4.30
CHEMBL3616567 — — 2 4.00
CHEMBL3616568 — — 2 4.00
CHEMBL3616569 — — 2 4.00
CHEMBL3616564 — — 2 -
CHEMBL3616553 — — 2 -
CHEMBL3616554 — — 2 -
CHEMBL3616579 — — 2 -
CHEMBL3616555 — — 2 -
CHEMBL3616556 — — 2 -
CHEMBL3616557 — — 2 -
CHEMBL3616558 — — 2 -
CHEMBL3616563 — — 2 -
CHEMBL3616478 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122270 LOBELINE Ki = 480.0 nM 6.32
CHEMBL122270 LOBELINE Ki = 501.19 nM 6.30
CHEMBL667 ACETYLCHOLINE Ki = 620.0 nM 6.21
CHEMBL667 ACETYLCHOLINE Ki = 616.6 nM 6.21
CHEMBL3616578 — Ki = 780.0 nM 6.11
CHEMBL3616578 — Ki = 776.25 nM 6.11
CHEMBL3616573 — Ki = 2200.0 nM 5.66
CHEMBL3616573 — Ki = 2187.76 nM 5.66
CHEMBL3616575 — Ki = 2570.4 nM 5.59
CHEMBL3616575 — Ki = 2600.0 nM 5.58
CHEMBL3616574 — Ki = 2900.0 nM 5.54
CHEMBL3616574 — Ki = 2951.21 nM 5.53
CHEMBL3616576 — Ki = 3388.44 nM 5.47
CHEMBL3616576 — Ki = 3400.0 nM 5.47
CHEMBL3616577 — Ki = 3800.0 nM 5.42
CHEMBL3616577 — Ki = 3801.89 nM 5.42
CHEMBL3616562 — Ki = 5900.0 nM 5.23
CHEMBL3616562 — Ki = 6025.6 nM 5.22
CHEMBL3616561 — Ki = 6900.0 nM 5.16
CHEMBL3616561 — Ki = 6918.31 nM 5.16
CHEMBL1090908 — Ki = 8200.0 nM 5.09
CHEMBL3616572 — Ki = 8300.0 nM 5.08
CHEMBL3616572 — Ki = 8317.64 nM 5.08
CHEMBL1090908 — Ki = 8317.64 nM 5.08
CHEMBL466400 — Ki = 10000.0 nM 5.00
CHEMBL466400 — Ki = 10471.29 nM 4.98
CHEMBL3616560 — Ki = 10715.19 nM 4.97
CHEMBL3616560 — Ki = 11000.0 nM 4.96
CHEMBL3616559 — Ki = 13000.0 nM 4.89
CHEMBL3616559 — Ki = 13182.57 nM 4.88
CHEMBL1090909 — Ki = 20000.0 nM 4.70
CHEMBL1090909 — Ki = 19952.62 nM 4.70
CHEMBL3616570 — Ki = 50000.0 nM 4.30
CHEMBL3616570 — Ki = 50118.72 nM 4.30
CHEMBL3616567 — Ki = 100000.0 nM 4.00
CHEMBL3616568 — Ki = 100000.0 nM 4.00
CHEMBL3616569 — Ki = 100000.0 nM 4.00
CHEMBL3616568 — Ki = 100000.0 nM 4.00
CHEMBL3616567 — Ki = 100000.0 nM 4.00
CHEMBL3616569 — Ki = 100000.0 nM 4.00
CHEMBL3616563 — Ki = 300000.0 nM -
CHEMBL3616564 — Ki = 300000.0 nM -
CHEMBL3616478 — Ki = 316227.77 nM -
CHEMBL3616558 — Ki > 1000000.0 nM -
CHEMBL3616557 — Ki = 1000000.0 nM -
CHEMBL3616565 — Ki = 300000.0 nM -
CHEMBL3616478 — Ki = 300000.0 nM -
CHEMBL3616571 — Ki > 316227.77 nM -
CHEMBL3616556 — Ki = 300000.0 nM -
CHEMBL3616579 — Ki > 316227.77 nM -