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Assay Detail

CHEMBL748018

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

Binding
Ability to displace radioligand [3H](-)-cytisine from Nicotinic acetylcholine receptor in rat brain membrane.
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Neuronal acetylcholine receptor (CHEMBL2094110)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-aminoethoxy)pyridine as novel nicotinic receptor ligands.
Lin NH, Dong L, Bunnelle WH, Anderson DJ, Meyer MD.
Bioorg Med Chem Lett (2002) 12 : 3321 -3324
PubMed 12392742 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 64 7.84 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419932 1 10.12
CHEMBL333162 1 10.11
CHEMBL112127 1 10.09
CHEMBL325352 1 10.00
CHEMBL112467 1 9.74
CHEMBL112254 1 9.43
CHEMBL113391 1 9.28
CHEMBL323696 1 9.24
CHEMBL115098 1 9.01
CHEMBL441650 1 8.82
CHEMBL323697 1 8.82
CHEMBL111935 1 8.82
CHEMBL113130 1 8.59
CHEMBL112316 1 8.44
CHEMBL432643 1 8.35
CHEMBL112961 1 8.34
CHEMBL109271 1 8.28
CHEMBL324939 1 8.26
CHEMBL114505 1 8.26
CHEMBL114881 1 8.23
CHEMBL109767 1 8.18
CHEMBL332720 1 8.15
CHEMBL113431 1 8.14
CHEMBL113240 1 8.06
CHEMBL320325 1 8.02
CHEMBL110202 1 8.00
CHEMBL111905 1 7.96
CHEMBL113260 1 7.96
CHEMBL324020 1 7.92
CHEMBL112989 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419932 Ki = 0.076 nM 10.12
CHEMBL333162 Ki = 0.077 nM 10.11
CHEMBL112127 Ki = 0.081 nM 10.09
CHEMBL325352 Ki = 0.1 nM 10.00
CHEMBL112467 Ki = 0.18 nM 9.74
CHEMBL112254 Ki = 0.37 nM 9.43
CHEMBL113391 Ki = 0.52 nM 9.28
CHEMBL323696 Ki = 0.57 nM 9.24
CHEMBL115098 Ki = 0.98 nM 9.01
CHEMBL441650 Ki = 1.5 nM 8.82
CHEMBL323697 Ki = 1.5 nM 8.82
CHEMBL111935 Ki = 1.5 nM 8.82
CHEMBL113130 Ki = 2.6 nM 8.59
CHEMBL112316 Ki = 3.6 nM 8.44
CHEMBL432643 Ki = 4.5 nM 8.35
CHEMBL112961 Ki = 4.6 nM 8.34
CHEMBL109271 Ki = 5.3 nM 8.28
CHEMBL324939 Ki = 5.5 nM 8.26
CHEMBL114505 Ki = 5.5 nM 8.26
CHEMBL114881 Ki = 5.9 nM 8.23
CHEMBL109767 Ki = 6.6 nM 8.18
CHEMBL332720 Ki = 7.1 nM 8.15
CHEMBL113431 Ki = 7.2 nM 8.14
CHEMBL113240 Ki = 8.7 nM 8.06
CHEMBL320325 Ki = 9.6 nM 8.02
CHEMBL110202 Ki = 9.9 nM 8.00
CHEMBL113260 Ki = 11.0 nM 7.96
CHEMBL111905 Ki = 11.0 nM 7.96
CHEMBL324020 Ki = 12.0 nM 7.92
CHEMBL112989 Ki = 13.0 nM 7.89
CHEMBL113295 Ki = 14.3 nM 7.84
CHEMBL113488 Ki = 15.0 nM 7.82
CHEMBL111821 Ki = 15.0 nM 7.82
CHEMBL326536 Ki = 16.0 nM 7.80
CHEMBL112221 Ki = 17.0 nM 7.77
CHEMBL113101 Ki = 22.0 nM 7.66
CHEMBL420496 Ki = 27.0 nM 7.57
CHEMBL112677 Ki = 31.0 nM 7.51
CHEMBL61616 Ki = 32.6 nM 7.49
CHEMBL325212 Ki = 37.0 nM 7.43
CHEMBL112471 Ki = 39.0 nM 7.41
CHEMBL112083 Ki = 41.0 nM 7.39
CHEMBL325898 Ki = 42.0 nM 7.38
CHEMBL112749 Ki = 42.0 nM 7.38
CHEMBL326918 Ki = 43.0 nM 7.37
CHEMBL115886 Ki = 50.0 nM 7.30
CHEMBL113319 Ki = 69.0 nM 7.16
CHEMBL112744 Ki = 70.0 nM 7.16
CHEMBL113076 Ki = 74.0 nM 7.13
CHEMBL326051 Ki = 79.0 nM 7.10