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Assay Detail

CHEMBL751265

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

Functional
Antagonistic activity against neuronal nicotinic acetylcholine receptor (alpha3-betaX subunit) in IMR 32 cell line using 100 uM of (-)-nicotine as agonist
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type IMR 32
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Nicotinic acetylcholine receptor alpha3/betaX (CHEMBL2111384)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.
Lin NH, Li Y, He Y, Holladay MW, Kuntzweiler T, Anderson DJ, Campbell JE, Arneric SP.
Bioorg Med Chem Lett (2001) 11 : 631 -633
PubMed 11266158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.48 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160950 1 6.16
CHEMBL346301 1 6.10
CHEMBL156204 1 6.10
CHEMBL157250 1 6.05
CHEMBL156502 1 5.96
CHEMBL345206 1 5.90
CHEMBL156049 1 5.82
CHEMBL349544 1 5.77
CHEMBL157188 1 5.70
CHEMBL352018 1 5.63
CHEMBL158834 1 5.63
CHEMBL159136 1 5.54
CHEMBL160624 1 5.47
CHEMBL158162 1 5.32
CHEMBL157135 1 5.29
CHEMBL156048 1 5.29
CHEMBL155909 1 5.24
CHEMBL347133 1 5.21
CHEMBL160766 1 5.20
CHEMBL158944 1 5.20
CHEMBL348275 1 5.19
CHEMBL158529 1 5.16
CHEMBL160447 1 5.16
CHEMBL156452 1 5.14
CHEMBL446684 1 5.12
CHEMBL158331 1 5.10
CHEMBL346981 1 4.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160950 IC50 = 690.0 nM 6.16
CHEMBL346301 IC50 = 790.0 nM 6.10
CHEMBL156204 IC50 = 800.0 nM 6.10
CHEMBL157250 IC50 = 890.0 nM 6.05
CHEMBL156502 IC50 = 1100.0 nM 5.96
CHEMBL345206 IC50 = 1250.0 nM 5.90
CHEMBL156049 IC50 = 1500.0 nM 5.82
CHEMBL349544 IC50 = 1700.0 nM 5.77
CHEMBL157188 IC50 = 1990.0 nM 5.70
CHEMBL352018 IC50 = 2350.0 nM 5.63
CHEMBL158834 IC50 = 2330.0 nM 5.63
CHEMBL159136 IC50 = 2900.0 nM 5.54
CHEMBL160624 IC50 = 3400.0 nM 5.47
CHEMBL158162 IC50 = 4800.0 nM 5.32
CHEMBL157135 IC50 = 5100.0 nM 5.29
CHEMBL156048 IC50 = 5100.0 nM 5.29
CHEMBL155909 IC50 = 5710.0 nM 5.24
CHEMBL347133 IC50 = 6100.0 nM 5.21
CHEMBL160766 IC50 = 6300.0 nM 5.20
CHEMBL158944 IC50 = 6310.0 nM 5.20
CHEMBL348275 IC50 = 6480.0 nM 5.19
CHEMBL158529 IC50 = 6900.0 nM 5.16
CHEMBL160447 IC50 = 6970.0 nM 5.16
CHEMBL156452 IC50 = 7300.0 nM 5.14
CHEMBL446684 IC50 = 7600.0 nM 5.12
CHEMBL158331 IC50 = 7900.0 nM 5.10
CHEMBL346981 IC50 = 24700.0 nM 4.61