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Assay Detail

CHEMBL779967

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

Functional
Effective concentration against rat aortic smooth muscle cell
27
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
Daugan A, Grondin P, Ruault C, Le Monnier de Gouville AC, Coste H, Linget JM, Kirilovsky J, Hyafil F, Labaudinière R.
J Med Chem (2003) 46 : 4533 -4542
PubMed 14521415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 6.25 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL779 TADALAFIL 4.0 2 6.82
CHEMBL434797 2 6.82
CHEMBL141703 1 6.70
CHEMBL334684 1 6.70
CHEMBL343941 1 6.52
CHEMBL342008 NORTADALAFIL 2 6.52
CHEMBL139597 1 6.46
CHEMBL336716 1 6.30
CHEMBL141307 1 6.30
CHEMBL138466 2 6.22
CHEMBL436019 1 6.22
CHEMBL342459 1 6.10
CHEMBL142143 1 6.00
CHEMBL138504 1 6.00
CHEMBL343553 1 5.82
CHEMBL140599 1 5.52
CHEMBL2111963 1 5.46
CHEMBL342876 1 -
CHEMBL445576 1 -
CHEMBL142138 1 -
CHEMBL344700 1 -
CHEMBL141518 1 -
CHEMBL343325 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434797 EC50 = 150.0 nM 6.82
CHEMBL779 TADALAFIL EC50 = 150.0 nM 6.82
CHEMBL334684 EC50 = 200.0 nM 6.70
CHEMBL141703 EC50 = 200.0 nM 6.70
CHEMBL342008 NORTADALAFIL EC50 = 300.0 nM 6.52
CHEMBL343941 EC50 = 300.0 nM 6.52
CHEMBL139597 EC50 = 350.0 nM 6.46
CHEMBL336716 EC50 = 500.0 nM 6.30
CHEMBL141307 EC50 = 500.0 nM 6.30
CHEMBL779 TADALAFIL EC50 = 500.0 nM 6.30
CHEMBL434797 EC50 = 500.0 nM 6.30
CHEMBL342008 NORTADALAFIL EC50 = 600.0 nM 6.22
CHEMBL138466 EC50 = 600.0 nM 6.22
CHEMBL436019 EC50 = 600.0 nM 6.22
CHEMBL342459 EC50 = 800.0 nM 6.10
CHEMBL138466 EC50 = 1000.0 nM 6.00
CHEMBL142143 EC50 = 1000.0 nM 6.00
CHEMBL138504 EC50 = 1000.0 nM 6.00
CHEMBL343553 EC50 = 1500.0 nM 5.82
CHEMBL140599 EC50 = 3000.0 nM 5.52
CHEMBL2111963 EC50 = 3500.0 nM 5.46
CHEMBL445576 EC50 > 10000.0 nM -
CHEMBL142138 EC50 > 10000.0 nM -
CHEMBL342876 EC50 > 10000.0 nM -
CHEMBL344700 EC50 > 10000.0 nM -
CHEMBL141518 EC50 > 10000.0 nM -
CHEMBL343325 EC50 > 10000.0 nM -