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Assay Detail

CHEMBL697539

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Binding
Binding affinity of compound against Histamine H3 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.
Kovalainen JT, Christiaans JA, Kotisaari S, Laitinen JT, Männistö PT, Tuomisto L, Gynther J.
J Med Chem (1999) 42 : 1193 -1202
PubMed 10197963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.35 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278462 CIPRALISANT 2.0 1 9.90
CHEMBL278276 1 9.40
CHEMBL13559 VUF-5296 1 8.50
CHEMBL18554 1 7.70
CHEMBL13795 VUF-5297 1 7.60
CHEMBL19469 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278462 CIPRALISANT Ki = 0.1259 nM 9.90
CHEMBL278276 Ki = 0.3981 nM 9.40
CHEMBL13559 VUF-5296 Ki = 3.162 nM 8.50
CHEMBL18554 Ki = 19.95 nM 7.70
CHEMBL13795 VUF-5297 Ki = 25.12 nM 7.60
CHEMBL19469 Ki = 100.0 nM 7.00