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Assay Detail

CHEMBL640806

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

Binding
Alpha adrenergic receptor activity in rat aorta
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Aorta
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and pharmacological properties of "soft drug" derivatives related to perhexiline.
Marciniak G, Decolin D, Leclerc G, Decker N, Schwartz J.
J Med Chem (1988) 31 : 2289 -2296
PubMed 2903931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 28 5.64 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1744096 1 6.70
CHEMBL75880 PERHEXILINE 4.0 1 6.70
CHEMBL75441 1 6.60
CHEMBL1201948 1 6.50
CHEMBL75664 1 6.50
CHEMBL1201949 1 6.15
CHEMBL1202832 1 6.10
CHEMBL76503 1 6.10
CHEMBL1201956 1 6.00
CHEMBL1744100 1 6.00
CHEMBL1744098 1 6.00
CHEMBL75665 1 6.00
CHEMBL1201955 1 5.90
CHEMBL76134 1 5.80
CHEMBL1201952 1 5.80
CHEMBL1201953 1 5.70
CHEMBL1202830 1 5.50
CHEMBL1201957 1 5.40
CHEMBL1201958 1 5.40
CHEMBL1202831 1 5.40
CHEMBL1744099 1 5.30
CHEMBL1744097 1 5.30
CHEMBL1201950 1 5.20
CHEMBL1744101 1 4.50
CHEMBL1744093 1 4.50
CHEMBL1201954 1 4.50
CHEMBL1201951 1 4.20
CHEMBL1744095 1 4.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1744096 Kd = 199.53 nM 6.70
CHEMBL75880 PERHEXILINE Kd = 199.53 nM 6.70
CHEMBL75441 Kd = 251.19 nM 6.60
CHEMBL1201948 Kd = 316.23 nM 6.50
CHEMBL75664 Kd = 316.23 nM 6.50
CHEMBL1201949 Kd = 707.95 nM 6.15
CHEMBL1202832 Kd = 794.33 nM 6.10
CHEMBL76503 Kd = 794.33 nM 6.10
CHEMBL1201956 Kd = 1000.0 nM 6.00
CHEMBL1744100 Kd = 1000.0 nM 6.00
CHEMBL1744098 Kd = 1000.0 nM 6.00
CHEMBL75665 Kd = 1000.0 nM 6.00
CHEMBL1201955 Kd = 1258.93 nM 5.90
CHEMBL76134 Kd = 1584.89 nM 5.80
CHEMBL1201952 Kd = 1584.89 nM 5.80
CHEMBL1201953 Kd = 1995.26 nM 5.70
CHEMBL1202830 Kd = 3162.28 nM 5.50
CHEMBL1201957 Kd = 3981.07 nM 5.40
CHEMBL1201958 Kd = 3981.07 nM 5.40
CHEMBL1202831 Kd = 3981.07 nM 5.40
CHEMBL1744099 Kd = 5011.87 nM 5.30
CHEMBL1744097 Kd = 5011.87 nM 5.30
CHEMBL1201950 Kd = 6309.57 nM 5.20
CHEMBL1744101 Kd = 31622.78 nM 4.50
CHEMBL1744093 Kd = 31622.78 nM 4.50
CHEMBL1201954 Kd = 31622.78 nM 4.50
CHEMBL1201951 Kd = 63095.73 nM 4.20
CHEMBL1744095 Kd = 79432.82 nM 4.10