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Assay Detail

CHEMBL4701950

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

Functional
Vasodilating activity in Sprague-Dawley rat aortic rings assessed as reduction in phenylephrine-induced contractions
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 1 — Organism
Curated By Autocuration

Target

Aorta (CHEMBL613606)
Type TISSUE
Organism Rattus norvegicus

Publication

Discovery of Novel Pyrazolo[3,4-b] Pyridine Derivatives with Dual Activities of Vascular Remodeling Inhibition and Vasodilation for the Treatment of Pulmonary Arterial Hypertension.
Hu L,Li L,Chang Q,Fu S,Qin J,Chen Z,Li X,Liu Q,Hu G,Li Q
J Med Chem (2020) 63 : 11215 -11234
PubMed 32914624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.79 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2107834 RIOCIGUAT 4.0 1 6.75
CHEMBL4785559 1 6.54
CHEMBL4743189 1 6.44
CHEMBL4792492 1 6.10
CHEMBL4795950 1 6.03
CHEMBL4797223 1 6.02
CHEMBL4752923 1 6.00
CHEMBL4782618 1 5.96
CHEMBL4780823 1 5.80
CHEMBL4783763 1 5.66
CHEMBL4761659 1 5.31
CHEMBL4761150 1 5.24
CHEMBL4763850 1 5.09
CHEMBL4752719 1 4.97
CHEMBL4784189 1 4.90
CHEMBL4749361 1 -
CHEMBL4754851 1 -
CHEMBL4782536 1 -
CHEMBL4795558 1 -
CHEMBL4749124 1 -
CHEMBL4764302 1 -
CHEMBL4745236 1 -
CHEMBL478629 DORSOMORPHIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2107834 RIOCIGUAT EC50 = 180.0 nM 6.75
CHEMBL4785559 EC50 = 290.0 nM 6.54
CHEMBL4743189 EC50 = 360.0 nM 6.44
CHEMBL4792492 EC50 = 790.0 nM 6.10
CHEMBL4795950 EC50 = 930.0 nM 6.03
CHEMBL4797223 EC50 = 960.0 nM 6.02
CHEMBL4752923 EC50 = 990.0 nM 6.00
CHEMBL4782618 EC50 = 1100.0 nM 5.96
CHEMBL4780823 EC50 = 1600.0 nM 5.80
CHEMBL4783763 EC50 = 2200.0 nM 5.66
CHEMBL4761659 EC50 = 4900.0 nM 5.31
CHEMBL4761150 EC50 = 5800.0 nM 5.24
CHEMBL4763850 EC50 = 8200.0 nM 5.09
CHEMBL4752719 EC50 = 10800.0 nM 4.97
CHEMBL4784189 EC50 = 12700.0 nM 4.90
CHEMBL4749361 EC50 > 100000.0 nM -
CHEMBL4754851 EC50 > 100000.0 nM -
CHEMBL4782536 EC50 > 100000.0 nM -
CHEMBL4795558 EC50 - -
CHEMBL4749124 EC50 - -
CHEMBL4764302 EC50 - -
CHEMBL4745236 EC50 - -
CHEMBL478629 DORSOMORPHIN EC50 - -