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Assay Detail

CHEMBL4337857

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

Binding
Binding affinity to 5-HT1A receptor (unknown origin) by radioligand displacement assay
1
Total Activities
1
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

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1<i>S</i>,3<i>R</i>)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1<i>H</i>)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA.
J Med Chem (2019) 62 : 8711 -8732
PubMed 31532644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.42 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3421729 MEVIDALEN 2.0 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3421729 MEVIDALEN IC50 = 3800.0 nM 5.42