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Assay Detail

CHEMBL646092

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

Binding
Binding affinity against Alpha-1D adrenergic receptor (recombinant human receptor) using [3H]-prazosin.
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.
Wong WC, Sun W, Lagu B, Tian D, Marzabadi MR, Zhang F, Nagarathnam D, Miao SW, Wetzel JM, Peng J, Forray C, Chang RS, Chen TB, Ransom R, O'Malley S, Broten TP, Kling P, Vyas KP, Zhang K, Gluchowski C.
J Med Chem (1999) 42 : 4804 -4813
PubMed 10579843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.29 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL145587 1 7.19
CHEMBL436407 1 7.10
CHEMBL145770 1 6.92
CHEMBL142981 1 6.82
CHEMBL145746 1 6.75
CHEMBL141322 3 6.75
CHEMBL359421 1 6.66
CHEMBL145411 1 6.36
CHEMBL144534 1 6.32
CHEMBL144731 1 6.24
CHEMBL357828 1 6.24
CHEMBL145278 1 6.21
CHEMBL5483012 1 6.20
CHEMBL141604 1 6.17
CHEMBL357842 1 6.16
CHEMBL145353 1 6.16
CHEMBL357131 1 6.04
CHEMBL142606 1 5.96
CHEMBL145001 1 5.96
CHEMBL145178 1 5.96
CHEMBL359430 1 5.80
CHEMBL342347 1 5.77
CHEMBL358313 1 5.77
CHEMBL142719 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL145587 Ki = 65.0 nM 7.19
CHEMBL436407 Ki = 79.0 nM 7.10
CHEMBL145770 Ki = 120.0 nM 6.92
CHEMBL142981 Ki = 150.0 nM 6.82
CHEMBL145746 Ki = 180.0 nM 6.75
CHEMBL141322 Ki = 180.0 nM 6.75
CHEMBL359421 Ki = 220.0 nM 6.66
CHEMBL145411 Ki = 440.0 nM 6.36
CHEMBL144534 Ki = 480.0 nM 6.32
CHEMBL141322 Ki = 550.0 nM 6.26
CHEMBL144731 Ki = 570.0 nM 6.24
CHEMBL357828 Ki = 580.0 nM 6.24
CHEMBL145278 Ki = 610.0 nM 6.21
CHEMBL5483012 Ki = 630.0 nM 6.20
CHEMBL141322 Ki = 680.0 nM 6.17
CHEMBL141604 Ki = 680.0 nM 6.17
CHEMBL145353 Ki = 690.0 nM 6.16
CHEMBL357842 Ki = 700.0 nM 6.16
CHEMBL357131 Ki = 910.0 nM 6.04
CHEMBL145001 Ki = 1100.0 nM 5.96
CHEMBL142606 Ki = 1100.0 nM 5.96
CHEMBL145178 Ki = 1100.0 nM 5.96
CHEMBL359430 Ki = 1600.0 nM 5.80
CHEMBL342347 Ki = 1700.0 nM 5.77
CHEMBL358313 Ki = 1700.0 nM 5.77
CHEMBL142719 Ki = 1900.0 nM 5.72