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Assay Detail

CHEMBL4406630

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

ADMET
Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cell membranes after 90 mins by microbeta scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H2 receptor (CHEMBL1941)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D3 Dopamine Receptor Agonist.
Moritz AE, Free RB, Weiner WS, Akano EO, Gandhi D, Abramyan A, Keck TM, Ferrer M, Hu X, Southall N, Steiner J, Aubé J, Shi L, Frankowski KJ, Sibley DR.
J Med Chem (2020) 63 : 5526 -5567
PubMed 32342685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.11 6.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203406 1 6.65
CHEMBL301265 PRAMIPEXOLE 4.0 1 5.57
CHEMBL4476784 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203406 Ki = 224.0 nM 6.65
CHEMBL301265 PRAMIPEXOLE Ki = 2683.0 nM 5.57
CHEMBL4476784 Ki - -