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Assay Detail

CHEMBL645683

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

Binding
In vitro binding affinity determined for alpha-1 adrenergic receptor by the displacement of [3H]- prazosin.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2,4-Diamino-6,7-dimethoxyquinazolines. 2. 2-(4-Carbamoylpiperidino) derivatives as alpha 1-adrenoceptor antagonists and antihypertensive agents.
Alabaster VA, Campbell SF, Danilewicz JC, Greengrass CW, Plews RM.
J Med Chem (1987) 30 : 999 -1003
PubMed 2884316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 9.04 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6424 1 10.00
CHEMBL2 PRAZOSIN 4.0 1 9.72
CHEMBL415288 1 9.70
CHEMBL6474 1 9.66
CHEMBL266317 1 9.38
CHEMBL267457 1 9.33
CHEMBL6380 1 9.33
CHEMBL6598 1 9.20
CHEMBL6766 1 9.19
CHEMBL6556 1 9.17
CHEMBL6481 1 9.10
CHEMBL6447 1 9.05
CHEMBL269537 1 8.97
CHEMBL267705 1 8.96
CHEMBL267164 1 8.95
CHEMBL6610 1 8.94
CHEMBL6789 1 8.85
CHEMBL266927 1 8.84
CHEMBL268627 1 8.79
CHEMBL6431 1 8.76
CHEMBL266279 1 8.08
CHEMBL6831 1 6.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6424 Ki = 0.1 nM 10.00
CHEMBL2 PRAZOSIN Ki = 0.19 nM 9.72
CHEMBL415288 Ki = 0.2 nM 9.70
CHEMBL6474 Ki = 0.22 nM 9.66
CHEMBL266317 Ki = 0.42 nM 9.38
CHEMBL267457 Ki = 0.47 nM 9.33
CHEMBL6380 Ki = 0.47 nM 9.33
CHEMBL6598 Ki = 0.63 nM 9.20
CHEMBL6766 Ki = 0.65 nM 9.19
CHEMBL6556 Ki = 0.67 nM 9.17
CHEMBL6481 Ki = 0.79 nM 9.10
CHEMBL6447 Ki = 0.9 nM 9.05
CHEMBL269537 Ki = 1.08 nM 8.97
CHEMBL267705 Ki = 1.11 nM 8.96
CHEMBL267164 Ki = 1.13 nM 8.95
CHEMBL6610 Ki = 1.14 nM 8.94
CHEMBL6789 Ki = 1.4 nM 8.85
CHEMBL266927 Ki = 1.46 nM 8.84
CHEMBL268627 Ki = 1.64 nM 8.79
CHEMBL6431 Ki = 1.73 nM 8.76
CHEMBL266279 Ki = 8.25 nM 8.08
CHEMBL6831 Ki = 116.73 nM 6.93