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Assay Detail

CHEMBL899886

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Functional
Agonist activity at recombinant human alpha-4-beta-2 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
ChEMBL ↗
110
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

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
EC50 110 5.86 7.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239961 — — 2 7.61
CHEMBL393246 — — 2 7.38
CHEMBL239959 — — 2 7.36
CHEMBL6623 EPIBATIDINE — 2 7.30
CHEMBL241665 — — 2 7.14
CHEMBL238712 — — 2 6.83
CHEMBL239960 — — 2 6.79
CHEMBL395936 — — 2 6.70
CHEMBL391166 — — 2 6.70
CHEMBL393627 — — 2 6.58
CHEMBL238448 — — 2 6.53
CHEMBL239505 — — 2 6.52
CHEMBL395174 — — 2 6.52
CHEMBL240371 — — 2 6.49
CHEMBL394109 — — 2 6.41
CHEMBL238465 SOFINICLINE 2.0 2 6.40
CHEMBL238670 — — 2 6.38
CHEMBL239504 — — 2 6.30
CHEMBL395935 — — 2 6.27
CHEMBL396138 — — 2 6.22
CHEMBL396308 — — 2 6.17
CHEMBL239742 — — 2 6.14
CHEMBL238710 — — 2 6.11
CHEMBL240372 — — 2 6.07
CHEMBL239721 — — 2 6.05
CHEMBL238672 — — 2 6.04
CHEMBL395456 — — 2 5.97
CHEMBL396310 — — 2 5.96
CHEMBL393247 — — 2 5.93
CHEMBL238673 — — 2 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239961 — EC50 = 24.55 nM 7.61
CHEMBL239961 — EC50 = 30.0 nM 7.52
CHEMBL393246 — EC50 = 41.69 nM 7.38
CHEMBL239959 — EC50 = 43.65 nM 7.36
CHEMBL6623 EPIBATIDINE EC50 = 50.0 nM 7.30
CHEMBL6623 EPIBATIDINE EC50 = 53.7 nM 7.27
CHEMBL241665 — EC50 = 72.44 nM 7.14
CHEMBL238712 — EC50 = 147.91 nM 6.83
CHEMBL239960 — EC50 = 162.18 nM 6.79
CHEMBL395936 — EC50 = 200.0 nM 6.70
CHEMBL238712 — EC50 = 200.0 nM 6.70
CHEMBL391166 — EC50 = 200.0 nM 6.70
CHEMBL239960 — EC50 = 200.0 nM 6.70
CHEMBL391166 — EC50 = 208.93 nM 6.68
CHEMBL395936 — EC50 = 229.09 nM 6.64
CHEMBL393627 — EC50 = 263.03 nM 6.58
CHEMBL238448 — EC50 = 295.12 nM 6.53
CHEMBL393627 — EC50 = 300.0 nM 6.52
CHEMBL239505 — EC50 = 300.0 nM 6.52
CHEMBL395174 — EC50 = 302.0 nM 6.52
CHEMBL395174 — EC50 = 300.0 nM 6.52
CHEMBL238448 — EC50 = 300.0 nM 6.52
CHEMBL239505 — EC50 = 323.59 nM 6.49
CHEMBL240371 — EC50 = 323.59 nM 6.49
CHEMBL394109 — EC50 = 389.05 nM 6.41
CHEMBL240371 — EC50 = 400.0 nM 6.40
CHEMBL394109 — EC50 = 400.0 nM 6.40
CHEMBL238465 SOFINICLINE EC50 = 400.0 nM 6.40
CHEMBL393246 — EC50 = 400.0 nM 6.40
CHEMBL238670 — EC50 = 416.87 nM 6.38
CHEMBL238465 SOFINICLINE EC50 = 446.68 nM 6.35
CHEMBL239504 — EC50 = 500.0 nM 6.30
CHEMBL239504 — EC50 = 501.19 nM 6.30
CHEMBL239959 — EC50 = 500.0 nM 6.30
CHEMBL395935 — EC50 = 537.03 nM 6.27
CHEMBL396138 — EC50 = 600.0 nM 6.22
CHEMBL395935 — EC50 = 600.0 nM 6.22
CHEMBL238670 — EC50 = 600.0 nM 6.22
CHEMBL396138 — EC50 = 616.6 nM 6.21
CHEMBL396308 — EC50 = 676.08 nM 6.17
CHEMBL241665 — EC50 = 700.0 nM 6.16
CHEMBL239742 — EC50 = 724.44 nM 6.14
CHEMBL238710 — EC50 = 776.25 nM 6.11
CHEMBL238710 — EC50 = 800.0 nM 6.10
CHEMBL239742 — EC50 = 800.0 nM 6.10
CHEMBL240372 — EC50 = 851.14 nM 6.07
CHEMBL239721 — EC50 = 900.0 nM 6.05
CHEMBL240372 — EC50 = 900.0 nM 6.05
CHEMBL239721 — EC50 = 912.01 nM 6.04
CHEMBL238672 — EC50 = 912.01 nM 6.04