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Assay Detail

CHEMBL678691

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

Binding
In vitro inhibition against autophosphorylation of Fibroblast growth factor receptor 2 in the human scirrhous gastric carcinoma cell line
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Fibroblast growth factor receptor 2 (CHEMBL4142)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.
Shimizu T, Fujiwara Y, Osawa T, Sakai T, Kubo K, Kubo K, Nishitoba T, Kimura K, Senga T, Murooka H, Iwai A, Fukushima K, Yoshino T, Miwa A.
Bioorg Med Chem Lett (2004) 14 : 875 -879
PubMed 15012985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.67 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL171509 1 7.64
CHEMBL170519 1 7.40
CHEMBL169837 1 7.27
CHEMBL170907 1 7.20
CHEMBL354898 1 7.16
CHEMBL414643 1 7.15
CHEMBL168335 1 7.15
CHEMBL352308 1 7.06
CHEMBL169854 1 7.00
CHEMBL167425 1 6.89
CHEMBL171413 1 6.72
CHEMBL354902 1 6.70
CHEMBL276125 1 6.70
CHEMBL169397 1 6.70
CHEMBL354224 1 6.58
CHEMBL355436 1 6.46
CHEMBL170415 1 6.36
CHEMBL354830 1 6.11
CHEMBL352534 1 5.47
CHEMBL352342 1 5.34
CHEMBL172746 1 5.05
CHEMBL353884 1 -
CHEMBL353668 1 -
CHEMBL171161 1 -
CHEMBL353991 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL171509 IC50 = 23.0 nM 7.64
CHEMBL170519 IC50 = 40.0 nM 7.40
CHEMBL169837 IC50 = 54.0 nM 7.27
CHEMBL170907 IC50 = 63.0 nM 7.20
CHEMBL354898 IC50 = 70.0 nM 7.16
CHEMBL414643 IC50 = 71.0 nM 7.15
CHEMBL168335 IC50 = 71.0 nM 7.15
CHEMBL352308 IC50 = 88.0 nM 7.06
CHEMBL169854 IC50 = 100.0 nM 7.00
CHEMBL167425 IC50 = 130.0 nM 6.89
CHEMBL171413 IC50 = 190.0 nM 6.72
CHEMBL354902 IC50 = 200.0 nM 6.70
CHEMBL276125 IC50 = 200.0 nM 6.70
CHEMBL169397 IC50 = 200.0 nM 6.70
CHEMBL354224 IC50 = 260.0 nM 6.58
CHEMBL355436 IC50 = 350.0 nM 6.46
CHEMBL170415 IC50 = 440.0 nM 6.36
CHEMBL354830 IC50 = 780.0 nM 6.11
CHEMBL352534 IC50 = 3400.0 nM 5.47
CHEMBL352342 IC50 = 4600.0 nM 5.34
CHEMBL172746 IC50 = 8900.0 nM 5.05
CHEMBL353884 IC50 > 10000.0 nM -
CHEMBL353668 IC50 > 1000.0 nM -
CHEMBL171161 IC50 > 10000.0 nM -
CHEMBL353991 IC50 > 10000.0 nM -