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Assay Detail

CHEMBL890276

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

Binding
Displacement of [3H]cytisine from alpha-4-beta-2 in rat cerebral cortical membrane
ChEMBL ↗
120
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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 studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.
Bunnelle WH, Daanen JF, Ryther KB, Schrimpf MR, Dart MJ, Gelain A, Meyer MD, Frost JM, Anderson DJ, Buckley M, Curzon P, Cao YJ, Puttfarcken P, Searle X, Ji J, Putman CB, Surowy C, Toma L, Barlocco D.
J Med Chem (2007) 50 : 3627 -3644
PubMed 17585748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 120 8.42 10.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388684 — — 2 10.87
CHEMBL388699 — — 2 10.74
CHEMBL389964 — — 4 10.74
CHEMBL245243 — — 4 10.74
CHEMBL389323 — — 2 10.70
CHEMBL242910 — — 4 10.57
CHEMBL395804 — — 4 10.55
CHEMBL436827 — — 4 10.46
CHEMBL6623 EPIBATIDINE — 2 10.33
CHEMBL243324 — — 2 10.33
CHEMBL243325 — — 2 10.19
CHEMBL430380 — — 2 10.00
CHEMBL242864 — — 4 9.92
CHEMBL242487 — — 4 9.77
CHEMBL243132 — — 2 9.70
CHEMBL340584 — — 4 9.62
CHEMBL243560 — — 2 9.60
CHEMBL390411 — — 2 9.08
CHEMBL395323 — — 4 9.08
CHEMBL3 NICOTINE 4.0 2 9.03
CHEMBL395325 — — 2 9.02
CHEMBL389965 — — 2 8.89
CHEMBL398004 — — 2 8.83
CHEMBL243344 — — 2 8.80
CHEMBL245259 — — 2 8.56
CHEMBL395324 — — 2 8.42
CHEMBL394572 — — 2 8.31
CHEMBL243530 — — 2 7.77
CHEMBL390214 — — 2 7.77
CHEMBL245048 — — 2 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388684 — Ki = 0.01349 nM 10.87
CHEMBL388684 — Ki = 0.014 nM 10.85
CHEMBL389964 — Ki = 0.0182 nM 10.74
CHEMBL245243 — Ki = 0.0182 nM 10.74
CHEMBL245243 — Ki = 0.018 nM 10.74
CHEMBL388699 — Ki = 0.0182 nM 10.74
CHEMBL388699 — Ki = 0.018 nM 10.74
CHEMBL389964 — Ki = 0.018 nM 10.74
CHEMBL389323 — Ki = 0.01995 nM 10.70
CHEMBL389323 — Ki = 0.02 nM 10.70
CHEMBL242910 — Ki = 0.027 nM 10.57
CHEMBL242910 — Ki = 0.02692 nM 10.57
CHEMBL395804 — Ki = 0.028 nM 10.55
CHEMBL395804 — Ki = 0.02818 nM 10.55
CHEMBL436827 — Ki = 0.035 nM 10.46
CHEMBL436827 — Ki = 0.03548 nM 10.45
CHEMBL243324 — Ki = 0.04677 nM 10.33
CHEMBL243324 — Ki = 0.047 nM 10.33
CHEMBL6623 EPIBATIDINE Ki = 0.04677 nM 10.33
CHEMBL6623 EPIBATIDINE Ki = 0.047 nM 10.33
CHEMBL243325 — Ki = 0.06457 nM 10.19
CHEMBL243325 — Ki = 0.065 nM 10.19
CHEMBL245243 — Ki = 0.1 nM 10.00
CHEMBL430380 — Ki = 0.1 nM 10.00
CHEMBL430380 — Ki = 0.1 nM 10.00
CHEMBL245243 — Ki = 0.1023 nM 9.99
CHEMBL242864 — Ki = 0.12 nM 9.92
CHEMBL242864 — Ki = 0.1259 nM 9.90
CHEMBL395804 — Ki = 0.1413 nM 9.85
CHEMBL389964 — Ki = 0.15 nM 9.82
CHEMBL389964 — Ki = 0.1549 nM 9.81
CHEMBL395804 — Ki = 0.17 nM 9.77
CHEMBL242487 — Ki = 0.17 nM 9.77
CHEMBL242487 — Ki = 0.1738 nM 9.76
CHEMBL243132 — Ki = 0.2 nM 9.70
CHEMBL243132 — Ki = 0.2042 nM 9.69
CHEMBL340584 — Ki = 0.24 nM 9.62
CHEMBL340584 — Ki = 0.2455 nM 9.61
CHEMBL243560 — Ki = 0.25 nM 9.60
CHEMBL243560 — Ki = 0.2512 nM 9.60
CHEMBL242864 — Ki = 0.5248 nM 9.28
CHEMBL242864 — Ki = 0.53 nM 9.28
CHEMBL390411 — Ki = 0.83 nM 9.08
CHEMBL390411 — Ki = 0.8318 nM 9.08
CHEMBL395323 — Ki = 0.83 nM 9.08
CHEMBL395323 — Ki = 0.8318 nM 9.08
CHEMBL3 NICOTINE Ki = 0.94 nM 9.03
CHEMBL3 NICOTINE Ki = 0.9333 nM 9.03
CHEMBL395325 — Ki = 0.95 nM 9.02
CHEMBL395325 — Ki = 0.955 nM 9.02