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Assay Detail

CHEMBL1100657

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

Binding
Displacement of [3H]histamine from histamine H3 receptor in rat cerebral cortex
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL4124)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
Łazewska D, Wiecek M, Ligneau X, Kottke T, Weizel L, Seifert R, Schunack W, Stark H, Kieć-Kononowicz K.
Bioorg Med Chem Lett (2009) 19 : 6682 -6685
PubMed 19846299 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.79 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1081718 1 8.29
CHEMBL1079552 1 8.06
CHEMBL1080263 1 7.92
CHEMBL1079554 1 7.92
CHEMBL1081541 1 7.82
CHEMBL1079748 1 7.75
CHEMBL1076300 1 7.75
CHEMBL1076275 1 7.75
CHEMBL1076267 1 7.75
CHEMBL1079553 1 7.72
CHEMBL1080089 1 7.72
CHEMBL1076266 1 7.70
CHEMBL1079746 1 7.66
CHEMBL1079918 1 7.64
CHEMBL1080090 1 7.64
CHEMBL1080262 1 7.60
CHEMBL1081719 1 -
CHEMBL1081720 1 -
CHEMBL1079747 1 -
CHEMBL1079749 1 -
CHEMBL1081912 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1081718 Ki = 5.1 nM 8.29
CHEMBL1079552 Ki = 8.7 nM 8.06
CHEMBL1080263 Ki = 12.0 nM 7.92
CHEMBL1079554 Ki = 12.0 nM 7.92
CHEMBL1081541 Ki = 15.0 nM 7.82
CHEMBL1079748 Ki = 18.0 nM 7.75
CHEMBL1076300 Ki = 18.0 nM 7.75
CHEMBL1076275 Ki = 18.0 nM 7.75
CHEMBL1076267 Ki = 18.0 nM 7.75
CHEMBL1079553 Ki = 19.0 nM 7.72
CHEMBL1080089 Ki = 19.0 nM 7.72
CHEMBL1076266 Ki = 20.0 nM 7.70
CHEMBL1079746 Ki = 22.0 nM 7.66
CHEMBL1079918 Ki = 23.0 nM 7.64
CHEMBL1080090 Ki = 23.0 nM 7.64
CHEMBL1080262 Ki = 25.0 nM 7.60
CHEMBL1081719 Ki - -
CHEMBL1081720 Ki - -
CHEMBL1079747 Ki - -
CHEMBL1079749 Ki - -
CHEMBL1081912 Ki - -