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Assay Detail

CHEMBL1120719

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

Binding
Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells
ChEMBL ↗
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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

In vitro studies on a class of quinoline containing histamine H3 antagonists.
Liu H, Altenbach RJ, Diaz GJ, Manelli AM, Martin RL, Miller TR, Esbenshade TA, Brioni JD, Cowart MD.
Bioorg Med Chem Lett (2010) 20 : 3295 -3300
PubMed 20457525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 75 5.64 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1082488 — — 1 7.52
CHEMBL1083463 — — 1 6.82
CHEMBL1086520 — — 1 6.66
CHEMBL1086513 — — 1 6.47
CHEMBL1084879 — — 1 6.42
CHEMBL1085396 — — 1 6.40
CHEMBL351231 — — 1 6.40
CHEMBL1084878 — — 1 6.40
CHEMBL1085142 — — 1 6.37
CHEMBL1085641 — — 1 6.36
CHEMBL1083562 — — 1 6.32
CHEMBL1086315 — — 1 6.32
CHEMBL1085124 — — 1 6.30
CHEMBL1085829 — — 1 6.21
CHEMBL1085336 — — 1 6.16
CHEMBL1086073 — — 1 6.15
CHEMBL1084383 — — 1 6.15
CHEMBL1086098 — — 1 6.14
CHEMBL1085800 — — 1 6.11
CHEMBL1083407 — — 1 6.06
CHEMBL1083448 — — 1 6.04
CHEMBL1086292 — — 1 6.03
CHEMBL1086534 — — 1 5.92
CHEMBL1085841 — — 1 5.92
CHEMBL1085572 — — 1 5.92
CHEMBL1084584 — — 1 5.82
CHEMBL1082606 — — 1 5.82
CHEMBL1085397 — — 1 5.82
CHEMBL1085398 — — 1 5.80
CHEMBL1085325 — — 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1082488 — Ki = 30.0 nM 7.52
CHEMBL1083463 — Ki = 150.0 nM 6.82
CHEMBL1086520 — Ki = 220.0 nM 6.66
CHEMBL1086513 — Ki = 340.0 nM 6.47
CHEMBL1084879 — Ki = 380.0 nM 6.42
CHEMBL1085396 — Ki = 400.0 nM 6.40
CHEMBL351231 — Ki = 400.0 nM 6.40
CHEMBL1084878 — Ki = 400.0 nM 6.40
CHEMBL1085142 — Ki = 430.0 nM 6.37
CHEMBL1085641 — Ki = 440.0 nM 6.36
CHEMBL1083562 — Ki = 480.0 nM 6.32
CHEMBL1086315 — Ki = 480.0 nM 6.32
CHEMBL1085124 — Ki = 500.0 nM 6.30
CHEMBL1085829 — Ki = 620.0 nM 6.21
CHEMBL1085336 — Ki = 690.0 nM 6.16
CHEMBL1086073 — Ki = 710.0 nM 6.15
CHEMBL1084383 — Ki = 710.0 nM 6.15
CHEMBL1086098 — Ki = 720.0 nM 6.14
CHEMBL1085800 — Ki = 780.0 nM 6.11
CHEMBL1083407 — Ki = 870.0 nM 6.06
CHEMBL1083448 — Ki = 910.0 nM 6.04
CHEMBL1086292 — Ki = 930.0 nM 6.03
CHEMBL1086534 — Ki = 1200.0 nM 5.92
CHEMBL1085841 — Ki = 1200.0 nM 5.92
CHEMBL1085572 — Ki = 1200.0 nM 5.92
CHEMBL1084584 — Ki = 1500.0 nM 5.82
CHEMBL1085397 — Ki = 1500.0 nM 5.82
CHEMBL1082606 — Ki = 1500.0 nM 5.82
CHEMBL1085398 — Ki = 1600.0 nM 5.80
CHEMBL1085325 — Ki = 1700.0 nM 5.77
CHEMBL1084385 — Ki = 2000.0 nM 5.70
CHEMBL1085326 — Ki = 2100.0 nM 5.68
CHEMBL1083447 — Ki = 2100.0 nM 5.68
CHEMBL1085560 — Ki = 2100.0 nM 5.68
CHEMBL392573 — Ki = 2200.0 nM 5.66
CHEMBL237394 — Ki = 2600.0 nM 5.58
CHEMBL237191 — Ki = 2600.0 nM 5.58
CHEMBL1085866 — Ki = 2800.0 nM 5.55
CHEMBL1086521 — Ki = 2900.0 nM 5.54
CHEMBL1084560 — Ki = 3000.0 nM 5.52
CHEMBL1086072 — Ki = 3100.0 nM 5.51
CHEMBL1084583 — Ki = 4200.0 nM 5.38
CHEMBL1084877 — Ki = 4200.0 nM 5.38
CHEMBL1084314 — Ki = 4400.0 nM 5.36
CHEMBL1082496 — Ki = 4500.0 nM 5.35
CHEMBL1083462 — Ki = 4500.0 nM 5.35
CHEMBL1082447 — Ki = 5000.0 nM 5.30
CHEMBL393581 — Ki = 5000.0 nM 5.30
CHEMBL1086514 — Ki = 5000.0 nM 5.30
CHEMBL1084294 — Ki = 5100.0 nM 5.29