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Assay Detail

CHEMBL647055

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

Binding
In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes
ChEMBL ↗
36
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Liver
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Murali Dhar TG, Nagarathnam D, Marzabadi MR, Lagu B, Wong WC, Chiu G, Tyagarajan S, Miao SW, Zhang F, Sun W, Tian D, Shen Q, Zhang J, Wetzel JM, Forray C, Chang RS, Broten TP, Schorn TW, Chen TB, O'Malley S, Ransom R, Schneck K, Bendesky R, Harrell CM, Vyas KP.
J Med Chem (1999) 42 : 4778 -4793
PubMed 10579841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 9.04 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL145894 — — 1 10.22
CHEMBL144933 — — 1 10.22
CHEMBL142929 — — 1 10.00
CHEMBL142981 — — 1 10.00
CHEMBL298713 — — 1 10.00
CHEMBL145459 — — 1 9.70
CHEMBL342126 — — 1 9.70
CHEMBL144925 — — 1 9.70
CHEMBL359012 — — 1 9.70
CHEMBL144938 — — 1 9.70
CHEMBL358785 — — 1 9.70
CHEMBL356584 — — 1 9.70
CHEMBL262217 — — 1 9.70
CHEMBL342543 — — 1 9.52
CHEMBL145170 — — 1 9.52
CHEMBL344339 — — 1 9.40
CHEMBL142243 — — 1 9.30
CHEMBL146109 — — 1 9.30
CHEMBL2 PRAZOSIN 4.0 1 9.22
CHEMBL357628 — — 1 9.15
CHEMBL144965 — — 1 9.00
CHEMBL424494 — — 1 8.96
CHEMBL145553 — — 1 8.77
CHEMBL144989 — — 1 8.72
CHEMBL145332 — — 1 8.49
CHEMBL358590 — — 2 8.38
CHEMBL342111 — — 1 8.35
CHEMBL145719 — — 1 8.34
CHEMBL145134 — — 1 8.28
CHEMBL611 TERAZOSIN 4.0 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL145894 — Ki = 0.06 nM 10.22
CHEMBL144933 — Ki = 0.06 nM 10.22
CHEMBL142981 — Ki = 0.1 nM 10.00
CHEMBL298713 — Ki = 0.1 nM 10.00
CHEMBL142929 — Ki = 0.1 nM 10.00
CHEMBL358785 — Ki = 0.2 nM 9.70
CHEMBL262217 — Ki = 0.2 nM 9.70
CHEMBL356584 — Ki = 0.2 nM 9.70
CHEMBL144938 — Ki = 0.2 nM 9.70
CHEMBL359012 — Ki = 0.2 nM 9.70
CHEMBL144925 — Ki = 0.2 nM 9.70
CHEMBL342126 — Ki = 0.2 nM 9.70
CHEMBL145459 — Ki = 0.2 nM 9.70
CHEMBL342543 — Ki = 0.3 nM 9.52
CHEMBL145170 — Ki = 0.3 nM 9.52
CHEMBL344339 — Ki = 0.4 nM 9.40
CHEMBL142243 — Ki = 0.5 nM 9.30
CHEMBL146109 — Ki = 0.5 nM 9.30
CHEMBL2 PRAZOSIN Ki = 0.6 nM 9.22
CHEMBL357628 — Ki = 0.7 nM 9.15
CHEMBL144965 — Ki = 1.0 nM 9.00
CHEMBL424494 — Ki = 1.1 nM 8.96
CHEMBL145553 — Ki = 1.7 nM 8.77
CHEMBL144989 — Ki = 1.9 nM 8.72
CHEMBL145332 — Ki = 3.2 nM 8.49
CHEMBL358590 — Ki = 4.2 nM 8.38
CHEMBL342111 — Ki = 4.5 nM 8.35
CHEMBL145719 — Ki = 4.6 nM 8.34
CHEMBL145134 — Ki = 5.2 nM 8.28
CHEMBL611 TERAZOSIN Ki = 6.9 nM 8.16
CHEMBL356571 — Ki = 6.9 nM 8.16
CHEMBL341838 — Ki = 7.5 nM 8.12
CHEMBL145571 — Ki = 7.9 nM 8.10
CHEMBL239806 — Ki = 19.0 nM 7.72
CHEMBL358590 — Ki = 58.0 nM 7.24
CHEMBL342064 — Ki = 81.0 nM 7.09