Assay Detail

CHEMBL1120225

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

Binding

Inhibition of human ERG

ChEMBL ↗

Free Research Context This assay will appear in recent viewed items on this browser. Open the demo workspace to preview project-only review queues.

Research home Demo workspace

Target

Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗

Open DB target context

Use one target anchor to keep assay intent, target linkage, and tested compound review aligned.

Loading context

Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Voltage-gated inwardly rectifying potassium channel KCNH2

CHEMBL240

Anchored from Assay target.

Protein identity Voltage-gated inwardly rectifying potassium channel KCNH2

Disease frame Disease evidence pending

Open the live target snapshot or evidence card before reviewing assay metadata so target fit and disease framing stay reusable.

Review focus Open DB context pending

Open the live target snapshot before relying on this target frame across surface handoff.

Open target snapshot Open evidence card Search with this context

Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.

Madsen-Duggan CB, Debenham JS, Walsh TF, Yan L, Huo P, Wang J, Tong X, Lao J, Fong TM, Xiao JC, Huang CR, Shen CP, Stribling DS, Shearman LP, Strack AM, Goulet MT, Hale JJ.
Bioorg Med Chem Lett (2010) 20 : 3750 -3754
PubMed 20483606 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	6.80	7.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1082330	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	—	1	7.40
CHEMBL1083646	(2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	—	1	6.92
CHEMBL1094521	—	—	1	6.47
CHEMBL1083025	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	—	1	6.42

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1082330	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	40.0	nM	7.40
CHEMBL1083646	(2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	120.0	nM	6.92
CHEMBL1094521	—	IC50	=	340.0	nM	6.47
CHEMBL1083025	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	380.0	nM	6.42