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Assay Detail

CHEMBL1168511

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Binding
Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane after 3 hrs
ChEMBL ↗
94
Total Activities
47
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

A computational study of the binding of 3-(arylidene) anabaseines to two major brain nicotinic acetylcholine receptors and to the acetylcholine binding protein.
Slavov SH, Radzvilovits M, LeFrancois S, Stoyanova-Slavova IB, Soti F, Kem WR, Katritzky AR.
Eur J Med Chem (2010) 45 : 2433 -2446
PubMed 20236734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pKi 47 - -
Ki 47 6.24 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1165581 — — 2 7.30
CHEMBL1164569 — — 2 7.22
CHEMBL1162395 — — 2 7.16
CHEMBL1163383 — — 2 6.92
CHEMBL1165544 — — 2 6.89
CHEMBL1165338 — — 2 6.80
CHEMBL1164492 — — 2 6.77
CHEMBL1165368 — — 2 6.77
CHEMBL1165604 — — 2 6.68
CHEMBL134713 GTS-21 2.0 2 6.60
CHEMBL1164686 — — 2 6.60
CHEMBL1165354 — — 2 6.55
CHEMBL1164015 — — 2 6.44
CHEMBL1164132 — — 2 6.42
CHEMBL1163793 — — 2 6.41
CHEMBL1163934 — — 2 6.37
CHEMBL1164116 — — 2 6.35
CHEMBL1164117 — — 2 6.31
CHEMBL1165617 — — 2 6.28
CHEMBL1165277 — — 2 6.28
CHEMBL1164471 — — 2 6.28
CHEMBL1165628 — — 2 6.22
CHEMBL1163432 — — 2 6.17
CHEMBL1165210 — — 2 6.16
CHEMBL1163448 — — 2 6.16
CHEMBL1165485 — — 2 6.11
CHEMBL1164133 — — 2 6.08
CHEMBL1164667 3-BENZYLIDENEANABASEINE — 2 6.07
CHEMBL1165179 — — 2 6.05
CHEMBL1164685 — — 2 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1165581 — Ki = 50.0 nM 7.30
CHEMBL1164569 — Ki = 60.0 nM 7.22
CHEMBL1162395 — Ki = 70.0 nM 7.16
CHEMBL1163383 — Ki = 120.0 nM 6.92
CHEMBL1165544 — Ki = 130.0 nM 6.89
CHEMBL1165338 — Ki = 160.0 nM 6.80
CHEMBL1165368 — Ki = 170.0 nM 6.77
CHEMBL1164492 — Ki = 170.0 nM 6.77
CHEMBL1165604 — Ki = 210.0 nM 6.68
CHEMBL1164686 — Ki = 250.0 nM 6.60
CHEMBL134713 GTS-21 Ki = 250.0 nM 6.60
CHEMBL1165354 — Ki = 280.0 nM 6.55
CHEMBL1164015 — Ki = 360.0 nM 6.44
CHEMBL1164132 — Ki = 380.0 nM 6.42
CHEMBL1163793 — Ki = 390.0 nM 6.41
CHEMBL1163934 — Ki = 430.0 nM 6.37
CHEMBL1164116 — Ki = 450.0 nM 6.35
CHEMBL1164117 — Ki = 490.0 nM 6.31
CHEMBL1165617 — Ki = 520.0 nM 6.28
CHEMBL1164471 — Ki = 520.0 nM 6.28
CHEMBL1165277 — Ki = 520.0 nM 6.28
CHEMBL1165628 — Ki = 600.0 nM 6.22
CHEMBL1163432 — Ki = 670.0 nM 6.17
CHEMBL1165210 — Ki = 700.0 nM 6.16
CHEMBL1163448 — Ki = 700.0 nM 6.16
CHEMBL1165485 — Ki = 770.0 nM 6.11
CHEMBL1164133 — Ki = 830.0 nM 6.08
CHEMBL1164667 3-BENZYLIDENEANABASEINE Ki = 850.0 nM 6.07
CHEMBL1164685 — Ki = 890.0 nM 6.05
CHEMBL1165179 — Ki = 900.0 nM 6.05
CHEMBL1163380 — Ki = 930.0 nM 6.03
CHEMBL1165185 — Ki = 970.0 nM 6.01
CHEMBL1163379 — Ki = 990.0 nM 6.00
CHEMBL1165786 — Ki = 1160.0 nM 5.94
CHEMBL1164724 — Ki = 1180.0 nM 5.93
CHEMBL1165521 — Ki = 1170.0 nM 5.93
CHEMBL1165180 — Ki = 1230.0 nM 5.91
CHEMBL1165557 — Ki = 1250.0 nM 5.90
CHEMBL1164221 — Ki = 1410.0 nM 5.85
CHEMBL1165301 — Ki = 1440.0 nM 5.84
CHEMBL1165211 — Ki = 1760.0 nM 5.75
CHEMBL1165460 — Ki = 1960.0 nM 5.71
CHEMBL1164115 — Ki = 2170.0 nM 5.66
CHEMBL1164787 — Ki = 4490.0 nM 5.35
CHEMBL1164570 — Ki = 4670.0 nM 5.33
CHEMBL1165121 — Ki = 5920.0 nM 5.23
CHEMBL1163934 — pKi = 0.367 uM -
CHEMBL1165121 — pKi = 0.772 uM -
CHEMBL1165628 — pKi = 0.222 uM -
CHEMBL1165604 — pKi = 0.678 uM -