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Assay Detail

CHEMBL899883

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

Binding
Displacement of [3H]cytisine from neuronal nicotinic acetylcholine receptor in rat brain membrane
ChEMBL ↗
114
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists.
Ji J, Schrimpf MR, Sippy KB, Bunnelle WH, Li T, Anderson DJ, Faltynek C, Surowy CS, Dyhring T, Ahring PK, Meyer MD.
J Med Chem (2007) 50 : 5493 -5508
PubMed 17929796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 114 9.11 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL241665 — — 2 10.40
CHEMBL393246 — — 2 10.40
CHEMBL6623 EPIBATIDINE — 2 10.33
CHEMBL239959 — — 2 10.22
CHEMBL395456 — — 2 10.20
CHEMBL238712 — — 2 10.15
CHEMBL395174 — — 2 10.10
CHEMBL238448 — — 2 10.00
CHEMBL238670 — — 2 10.00
CHEMBL238672 — — 2 10.00
CHEMBL239961 — — 2 9.77
CHEMBL395936 — — 2 9.70
CHEMBL394109 — — 2 9.70
CHEMBL396138 — — 2 9.70
CHEMBL240372 — — 2 9.70
CHEMBL240371 — — 2 9.60
CHEMBL391166 — — 2 9.59
CHEMBL393627 — — 2 9.55
CHEMBL238465 SOFINICLINE 2.0 2 9.53
CHEMBL393247 — — 2 9.52
CHEMBL238710 — — 2 9.52
CHEMBL396308 — — 2 9.35
CHEMBL239960 — — 2 9.24
CHEMBL391554 — — 2 9.22
CHEMBL239742 — — 2 9.22
CHEMBL239504 — — 2 9.18
CHEMBL238452 — — 2 9.15
CHEMBL239932 — — 2 9.12
CHEMBL239931 — — 2 9.07
CHEMBL3 NICOTINE 4.0 2 9.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL393246 — Ki = 0.03981 nM 10.40
CHEMBL393246 — Ki = 0.04 nM 10.40
CHEMBL241665 — Ki = 0.03981 nM 10.40
CHEMBL241665 — Ki = 0.04 nM 10.40
CHEMBL6623 EPIBATIDINE Ki = 0.04677 nM 10.33
CHEMBL6623 EPIBATIDINE Ki = 0.05 nM 10.30
CHEMBL239959 — Ki = 0.06 nM 10.22
CHEMBL239959 — Ki = 0.06026 nM 10.22
CHEMBL395456 — Ki = 0.0631 nM 10.20
CHEMBL238712 — Ki = 0.07 nM 10.15
CHEMBL238712 — Ki = 0.07079 nM 10.15
CHEMBL395174 — Ki = 0.08 nM 10.10
CHEMBL395174 — Ki = 0.07943 nM 10.10
CHEMBL238448 — Ki = 0.1 nM 10.00
CHEMBL238672 — Ki = 0.1 nM 10.00
CHEMBL238670 — Ki = 0.1 nM 10.00
CHEMBL395456 — Ki = 0.1 nM 10.00
CHEMBL238448 — Ki = 0.1096 nM 9.96
CHEMBL238672 — Ki = 0.1096 nM 9.96
CHEMBL238670 — Ki = 0.1202 nM 9.92
CHEMBL239961 — Ki = 0.1698 nM 9.77
CHEMBL396138 — Ki = 0.2 nM 9.70
CHEMBL396138 — Ki = 0.1995 nM 9.70
CHEMBL394109 — Ki = 0.2 nM 9.70
CHEMBL239961 — Ki = 0.2 nM 9.70
CHEMBL240372 — Ki = 0.2 nM 9.70
CHEMBL395936 — Ki = 0.1995 nM 9.70
CHEMBL395936 — Ki = 0.2 nM 9.70
CHEMBL240372 — Ki = 0.2089 nM 9.68
CHEMBL394109 — Ki = 0.2399 nM 9.62
CHEMBL240371 — Ki = 0.2512 nM 9.60
CHEMBL391166 — Ki = 0.257 nM 9.59
CHEMBL393627 — Ki = 0.2818 nM 9.55
CHEMBL238465 SOFINICLINE Ki = 0.2951 nM 9.53
CHEMBL238465 SOFINICLINE Ki = 0.3 nM 9.52
CHEMBL393247 — Ki = 0.3 nM 9.52
CHEMBL393247 — Ki = 0.302 nM 9.52
CHEMBL393627 — Ki = 0.3 nM 9.52
CHEMBL238710 — Ki = 0.3 nM 9.52
CHEMBL240371 — Ki = 0.3 nM 9.52
CHEMBL391166 — Ki = 0.3 nM 9.52
CHEMBL238710 — Ki = 0.309 nM 9.51
CHEMBL396308 — Ki = 0.4467 nM 9.35
CHEMBL396308 — Ki = 0.5 nM 9.30
CHEMBL239960 — Ki = 0.5754 nM 9.24
CHEMBL239742 — Ki = 0.6 nM 9.22
CHEMBL391554 — Ki = 0.6 nM 9.22
CHEMBL239960 — Ki = 0.6 nM 9.22
CHEMBL391554 — Ki = 0.6166 nM 9.21
CHEMBL239742 — Ki = 0.631 nM 9.20