Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL748859

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

Binding
Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 in rat brain using [3H]-cytisine as radioligand
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.
Holladay MW, Bai H, Li Y, Lin NH, Daanen JF, Ryther KB, Wasicak JT, Kincaid JF, He Y, Hettinger AM, Huang P, Anderson DJ, Bannon AW, Buckley MJ, Campbell JE, Donnelly-Roberts DL, Gunther KL, Kim DJ, Kuntzweiler TA, Sullivan JP, Decker MW, Arneric SP.
Bioorg Med Chem Lett (1998) 8 : 2797 -2802
PubMed 9873625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 9.52 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317087 — — 1 10.82
CHEMBL407258 — — 1 10.68
CHEMBL318869 — — 1 10.66
CHEMBL97555 — — 1 10.64
CHEMBL94683 — — 1 10.60
CHEMBL96604 — — 1 10.41
CHEMBL96837 — — 1 10.41
CHEMBL439766 — — 1 10.40
CHEMBL430497 TEBANICLINE 2.0 1 10.40
CHEMBL95113 — — 1 10.38
CHEMBL96201 — — 1 10.34
CHEMBL96431 — — 1 10.33
CHEMBL308538 — — 1 10.32
CHEMBL94670 — — 1 10.28
CHEMBL59986 — — 1 10.28
CHEMBL318121 — — 1 10.24
CHEMBL94877 — — 1 10.24
CHEMBL446410 — — 1 10.18
CHEMBL96527 — — 1 10.12
CHEMBL94207 — — 1 10.09
CHEMBL95128 — — 1 10.06
CHEMBL96370 — — 1 10.00
CHEMBL95132 — — 1 9.92
CHEMBL97314 — — 1 9.80
CHEMBL314303 — — 1 9.77
CHEMBL96733 — — 1 9.74
CHEMBL317486 — — 1 9.48
CHEMBL318726 — — 1 9.40
CHEMBL96630 — — 1 9.31
CHEMBL94528 — — 1 9.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317087 — Ki = 0.015 nM 10.82
CHEMBL407258 — Ki = 0.021 nM 10.68
CHEMBL318869 — Ki = 0.022 nM 10.66
CHEMBL97555 — Ki = 0.023 nM 10.64
CHEMBL94683 — Ki = 0.025 nM 10.60
CHEMBL96604 — Ki = 0.039 nM 10.41
CHEMBL96837 — Ki = 0.039 nM 10.41
CHEMBL439766 — Ki = 0.04 nM 10.40
CHEMBL430497 TEBANICLINE Ki = 0.04 nM 10.40
CHEMBL95113 — Ki = 0.042 nM 10.38
CHEMBL96201 — Ki = 0.046 nM 10.34
CHEMBL96431 — Ki = 0.047 nM 10.33
CHEMBL308538 — Ki = 0.048 nM 10.32
CHEMBL94670 — Ki = 0.053 nM 10.28
CHEMBL59986 — Ki = 0.052 nM 10.28
CHEMBL318121 — Ki = 0.057 nM 10.24
CHEMBL94877 — Ki = 0.057 nM 10.24
CHEMBL446410 — Ki = 0.066 nM 10.18
CHEMBL96527 — Ki = 0.076 nM 10.12
CHEMBL94207 — Ki = 0.082 nM 10.09
CHEMBL95128 — Ki = 0.088 nM 10.06
CHEMBL96370 — Ki = 0.1 nM 10.00
CHEMBL95132 — Ki = 0.12 nM 9.92
CHEMBL97314 — Ki = 0.16 nM 9.80
CHEMBL314303 — Ki = 0.17 nM 9.77
CHEMBL96733 — Ki = 0.18 nM 9.74
CHEMBL317486 — Ki = 0.33 nM 9.48
CHEMBL318726 — Ki = 0.4 nM 9.40
CHEMBL96630 — Ki = 0.49 nM 9.31
CHEMBL94528 — Ki = 0.54 nM 9.27
CHEMBL94304 — Ki = 0.67 nM 9.17
CHEMBL92038 — Ki = 1.25 nM 8.90
CHEMBL97288 — Ki = 1.3 nM 8.89
CHEMBL441069 — Ki = 1.36 nM 8.87
CHEMBL327164 — Ki = 1.9 nM 8.72
CHEMBL94843 — Ki = 2.3 nM 8.64
CHEMBL95154 — Ki = 2.3 nM 8.64
CHEMBL94853 — Ki = 2.4 nM 8.62
CHEMBL94626 — Ki = 4.4 nM 8.36
CHEMBL97482 — Ki = 7.6 nM 8.12
CHEMBL318227 — Ki = 12.0 nM 7.92
CHEMBL94942 — Ki = 19.0 nM 7.72
CHEMBL96136 — Ki = 37.0 nM 7.43
CHEMBL432216 — Ki = 85.0 nM 7.07
CHEMBL93934 — Ki = 260.0 nM 6.58