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Assay Detail

CHEMBL832611

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

Binding
In vitro insecticidal activity as inhibition of [3H]EBOB binding to Gamma-aminobutyric acid GABA-A receptor of housefly neuronal membranes
38
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Musca domestica
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2093872)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles.
Meegalla SK, Doller D, Sha D, Soll R, Wisnewski N, Silver GM, Dhanoa D.
Bioorg Med Chem Lett (2004) 14 : 4949 -4953
PubMed 15341958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.83 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101326 FIPRONIL -1.0 1 8.64
CHEMBL366062 1 8.38
CHEMBL2112054 1 8.10
CHEMBL128970 1 8.10
CHEMBL184173 1 7.64
CHEMBL181500 1 7.60
CHEMBL184495 1 7.58
CHEMBL183157 1 7.37
CHEMBL445138 1 7.30
CHEMBL359769 1 7.28
CHEMBL186772 1 7.06
CHEMBL364173 1 7.05
CHEMBL182710 1 7.05
CHEMBL363671 1 6.98
CHEMBL187912 1 6.96
CHEMBL184619 1 6.92
CHEMBL362308 1 6.91
CHEMBL434522 1 6.82
CHEMBL185214 2 6.80
CHEMBL184176 1 6.80
CHEMBL277106 1 6.77
CHEMBL424805 1 6.52
CHEMBL185204 1 6.49
CHEMBL364148 1 6.46
CHEMBL188113 1 6.42
CHEMBL184150 1 6.40
CHEMBL184570 2 6.40
CHEMBL359971 1 6.30
CHEMBL181760 1 6.30
CHEMBL187479 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101326 FIPRONIL IC50 = 2.3 nM 8.64
CHEMBL366062 IC50 = 4.2 nM 8.38
CHEMBL128970 IC50 = 8.0 nM 8.10
CHEMBL2112054 IC50 = 8.0 nM 8.10
CHEMBL184173 IC50 = 23.0 nM 7.64
CHEMBL181500 IC50 = 25.0 nM 7.60
CHEMBL184495 IC50 = 26.0 nM 7.58
CHEMBL183157 IC50 = 43.0 nM 7.37
CHEMBL445138 IC50 = 50.0 nM 7.30
CHEMBL359769 IC50 = 52.0 nM 7.28
CHEMBL186772 IC50 = 87.0 nM 7.06
CHEMBL364173 IC50 = 90.0 nM 7.05
CHEMBL182710 IC50 = 90.0 nM 7.05
CHEMBL363671 IC50 = 105.0 nM 6.98
CHEMBL187912 IC50 = 110.0 nM 6.96
CHEMBL184619 IC50 = 120.0 nM 6.92
CHEMBL362308 IC50 = 124.0 nM 6.91
CHEMBL434522 IC50 = 150.0 nM 6.82
CHEMBL184176 IC50 = 160.0 nM 6.80
CHEMBL185214 IC50 = 160.0 nM 6.80
CHEMBL277106 IC50 = 170.0 nM 6.77
CHEMBL424805 IC50 = 300.0 nM 6.52
CHEMBL185204 IC50 = 325.0 nM 6.49
CHEMBL364148 IC50 = 350.0 nM 6.46
CHEMBL188113 IC50 = 380.0 nM 6.42
CHEMBL184150 IC50 = 400.0 nM 6.40
CHEMBL185214 IC50 = 400.0 nM 6.40
CHEMBL184570 IC50 = 400.0 nM 6.40
CHEMBL359971 IC50 = 500.0 nM 6.30
CHEMBL181760 IC50 = 500.0 nM 6.30
CHEMBL187479 IC50 = 700.0 nM 6.16
CHEMBL365495 IC50 = 700.0 nM 6.16
CHEMBL186607 IC50 = 740.0 nM 6.13
CHEMBL184494 IC50 = 800.0 nM 6.10
CHEMBL360215 IC50 = 1000.0 nM 6.00
CHEMBL365218 IC50 = 1000.0 nM 6.00
CHEMBL187911 IC50 = 1500.0 nM 5.82
CHEMBL184570 IC50 = 4000.0 nM 5.40