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Assay Detail

CHEMBL989048

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

Binding
Binding affinity to 5HT1A receptor
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
Cowart MD, Altenbach RJ, Liu H, Hsieh GC, Drizin I, Milicic I, Miller TR, Witte DG, Wishart N, Fix-Stenzel SR, McPherson MJ, Adair RM, Wetter JM, Bettencourt BM, Marsh KC, Sullivan JP, Honore P, Esbenshade TA, Brioni JD.
J Med Chem (2008) 51 : 6547 -6557
PubMed 18817367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.38 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494678 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494678 Ki = 42.0 nM 7.38