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Assay Detail

CHEMBL633442

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ADMET
pA2 value is determined compared to standard H1-antagonists
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.
Abou-Gharbia M, Moyer JA, Nielsen ST, Webb M, Patel U.
J Med Chem (1995) 38 : 4026 -4032
PubMed 7562938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.96 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL505 CHLORPHENIRAMINE 4.0 1 8.40
CHEMBL296419 ASTEMIZOLE 4.0 1 8.30
CHEMBL553331 1 8.20
CHEMBL17157 TERFENADINE 4.0 1 7.50
CHEMBL305660 EBASTINE 4.0 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL505 CHLORPHENIRAMINE Kd = 3.981 nM 8.40
CHEMBL296419 ASTEMIZOLE Kd = 5.012 nM 8.30
CHEMBL553331 Kd = 6.31 nM 8.20
CHEMBL17157 TERFENADINE Kd = 31.62 nM 7.50
CHEMBL305660 EBASTINE Kd = 39.81 nM 7.40