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Assay Detail

CHEMBL861464

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Functional
Antiproliferative activity against PDGF-BB stimulated HCASMC
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Platelet-derived growth factor receptor beta (CHEMBL1913)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.
Ho CY, Ludovici DW, Maharoof US, Mei J, Sechler JL, Tuman RW, Strobel ED, Andraka L, Yen HK, Leo G, Li J, Almond H, Lu H, DeVine A, Tominovich RM, Baker J, Emanuel S, Gruninger RH, Middleton SA, Johnson DL, Galemmo RA.
J Med Chem (2005) 48 : 8163 -8173
PubMed 16366598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.54 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184948 1 9.00
CHEMBL120077 1 8.52
CHEMBL371949 1 8.05
CHEMBL332375 1 7.96
CHEMBL120634 1 7.80
CHEMBL432219 1 7.64
CHEMBL120862 1 7.50
CHEMBL121161 1 6.91
CHEMBL331760 1 6.73
CHEMBL200735 1 6.57
CHEMBL371910 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184948 IC50 = 1.0 nM 9.00
CHEMBL120077 IC50 = 3.0 nM 8.52
CHEMBL371949 IC50 = 9.0 nM 8.05
CHEMBL332375 IC50 = 11.0 nM 7.96
CHEMBL120634 IC50 = 16.0 nM 7.80
CHEMBL432219 IC50 = 23.0 nM 7.64
CHEMBL120862 IC50 = 32.0 nM 7.50
CHEMBL121161 IC50 = 124.0 nM 6.91
CHEMBL331760 IC50 = 188.0 nM 6.73
CHEMBL200735 IC50 = 268.0 nM 6.57
CHEMBL371910 IC50 = 487.0 nM 6.31