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Assay Detail

CHEMBL1107671

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

Binding
Displacement of [3H]dofetidile from human ERG by scintillation proximity assay
ChEMBL ↗
105
Total Activities
54
Compounds Tested
1
Activity Types
0
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

1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists.
Micheli F, Arista L, Bonanomi G, Blaney FE, Braggio S, Capelli AM, Checchia A, Damiani F, Di-Fabio R, Fontana S, Gentile G, Griffante C, Hamprecht D, Marchioro C, Mugnaini M, Piner J, Ratti E, Tedesco G, Tarsi L, Terreni S, Worby A, Ashby CR, Heidbreder C.
J Med Chem (2010) 53 : 374 -391
PubMed 19891474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 105 5.97 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1079497 — — 1 6.90
CHEMBL1080293 — — 1 6.80
CHEMBL1079639 — — 1 6.70
CHEMBL1080117 — — 3 6.70
CHEMBL1081966 — — 3 6.70
CHEMBL1080165 — — 1 6.60
CHEMBL1081401 — — 3 6.60
CHEMBL1079461 — — 3 6.50
CHEMBL1079462 — — 3 6.50
CHEMBL1080490 — — 3 6.40
CHEMBL1082106 — — 3 6.40
CHEMBL1081747 — — 3 6.40
CHEMBL1079814 — — 1 6.40
CHEMBL1079823 — — 1 6.40
CHEMBL1080126 — — 3 6.40
CHEMBL1081587 — — 3 6.30
CHEMBL1080846 — — 3 6.30
CHEMBL1080164 — — 1 6.30
CHEMBL1081685 — — 1 6.30
CHEMBL1081023 — — 3 6.30
CHEMBL1081934 — — 3 6.20
CHEMBL1081686 — — 1 6.20
CHEMBL1079577 — — 1 6.20
CHEMBL1081580 — — 1 6.20
CHEMBL1081237 — — 3 6.20
CHEMBL1079822 — — 1 6.20
CHEMBL1079578 — — 3 6.20
CHEMBL1079494 — — 3 6.10
CHEMBL1079640 — — 1 6.10
CHEMBL1079480 — — 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1079497 — IC50 = 125.89 nM 6.90
CHEMBL1080293 — IC50 = 158.49 nM 6.80
CHEMBL1081966 — IC50 = 199.53 nM 6.70
CHEMBL1079639 — IC50 = 199.53 nM 6.70
CHEMBL1080117 — IC50 = 199.53 nM 6.70
CHEMBL1081966 — IC50 = 251.19 nM 6.60
CHEMBL1080165 — IC50 = 251.19 nM 6.60
CHEMBL1081401 — IC50 = 251.19 nM 6.60
CHEMBL1081401 — IC50 = 251.19 nM 6.60
CHEMBL1081401 — IC50 = 251.19 nM 6.60
CHEMBL1079462 — IC50 = 316.23 nM 6.50
CHEMBL1079461 — IC50 = 316.23 nM 6.50
CHEMBL1081966 — IC50 = 316.23 nM 6.50
CHEMBL1081747 — IC50 = 398.11 nM 6.40
CHEMBL1080126 — IC50 = 398.11 nM 6.40
CHEMBL1079814 — IC50 = 398.11 nM 6.40
CHEMBL1080490 — IC50 = 398.11 nM 6.40
CHEMBL1082106 — IC50 = 398.11 nM 6.40
CHEMBL1079823 — IC50 = 398.11 nM 6.40
CHEMBL1080164 — IC50 = 501.19 nM 6.30
CHEMBL1081685 — IC50 = 501.19 nM 6.30
CHEMBL1082106 — IC50 = 501.19 nM 6.30
CHEMBL1081023 — IC50 = 501.19 nM 6.30
CHEMBL1081587 — IC50 = 501.19 nM 6.30
CHEMBL1081747 — IC50 = 501.19 nM 6.30
CHEMBL1080846 — IC50 = 501.19 nM 6.30
CHEMBL1081686 — IC50 = 630.96 nM 6.20
CHEMBL1081934 — IC50 = 630.96 nM 6.20
CHEMBL1080126 — IC50 = 630.96 nM 6.20
CHEMBL1080126 — IC50 = 630.96 nM 6.20
CHEMBL1079822 — IC50 = 630.96 nM 6.20
CHEMBL1079578 — IC50 = 630.96 nM 6.20
CHEMBL1079578 — IC50 = 630.96 nM 6.20
CHEMBL1079577 — IC50 = 630.96 nM 6.20
CHEMBL1081237 — IC50 = 630.96 nM 6.20
CHEMBL1081580 — IC50 = 630.96 nM 6.20
CHEMBL1081409 — IC50 = 794.33 nM 6.10
CHEMBL1080490 — IC50 = 794.33 nM 6.10
CHEMBL1079494 — IC50 = 794.33 nM 6.10
CHEMBL1081023 — IC50 = 794.33 nM 6.10
CHEMBL1080490 — IC50 = 794.33 nM 6.10
CHEMBL1082106 — IC50 = 794.33 nM 6.10
CHEMBL1079480 — IC50 = 794.33 nM 6.10
CHEMBL1079640 — IC50 = 794.33 nM 6.10
CHEMBL1081203 — IC50 = 794.33 nM 6.10
CHEMBL1081934 — IC50 = 1000.0 nM 6.00
CHEMBL1079938 — IC50 = 1000.0 nM 6.00
CHEMBL1081868 — IC50 = 1000.0 nM 6.00
CHEMBL1081869 — IC50 = 1000.0 nM 6.00
CHEMBL1081747 — IC50 = 1000.0 nM 6.00