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Assay Detail

CHEMBL678675

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Binding
Inhibitory concentration evaluated against fibroblast growth factor receptor 1.
ChEMBL ↗
54
Total Activities
54
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 1 (CHEMBL3650) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.
Klutchko SR, Hamby JM, Boschelli DH, Wu Z, Kraker AJ, Amar AM, Hartl BG, Shen C, Klohs WD, Steinkampf RW, Driscoll DL, Nelson JM, Elliott WL, Roberts BJ, Stoner CL, Vincent PW, Dykes DJ, Panek RL, Lu GH, Major TC, Dahring TK, Hallak H, Bradford LA, Showalter HD, Doherty AM.
J Med Chem (1998) 41 : 3276 -3292
PubMed 9703473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 6.32 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51283 — — 1 7.55
CHEMBL297523 — — 1 7.50
CHEMBL110905 — — 1 7.48
CHEMBL112080 — — 1 7.47
CHEMBL323775 — — 1 7.41
CHEMBL324543 — — 1 7.40
CHEMBL320339 — — 1 7.34
CHEMBL112706 — — 1 7.31
CHEMBL331366 — — 1 7.26
CHEMBL50647 — — 1 7.21
CHEMBL113521 — — 1 7.18
CHEMBL327127 — — 1 7.10
CHEMBL113070 — — 1 6.96
CHEMBL448154 — — 1 6.96
CHEMBL109631 — — 1 6.96
CHEMBL325589 — — 1 6.82
CHEMBL323405 — — 1 6.82
CHEMBL321193 — — 1 6.75
CHEMBL104779 — — 1 6.72
CHEMBL322298 — — 1 6.68
CHEMBL106232 — — 1 6.62
CHEMBL104244 — — 1 6.50
CHEMBL111197 — — 1 6.43
CHEMBL299194 — — 1 6.42
CHEMBL104153 — — 1 6.39
CHEMBL324926 — — 1 6.37
CHEMBL113023 — — 1 6.35
CHEMBL301612 — — 1 6.34
CHEMBL111365 — — 1 6.27
CHEMBL113863 — — 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51283 — IC50 = 28.0 nM 7.55
CHEMBL297523 — IC50 = 32.0 nM 7.50
CHEMBL110905 — IC50 = 33.0 nM 7.48
CHEMBL112080 — IC50 = 34.0 nM 7.47
CHEMBL323775 — IC50 = 39.0 nM 7.41
CHEMBL324543 — IC50 = 40.0 nM 7.40
CHEMBL320339 — IC50 = 46.0 nM 7.34
CHEMBL112706 — IC50 = 49.0 nM 7.31
CHEMBL331366 — IC50 = 55.0 nM 7.26
CHEMBL50647 — IC50 = 61.0 nM 7.21
CHEMBL113521 — IC50 = 66.0 nM 7.18
CHEMBL327127 — IC50 = 80.0 nM 7.10
CHEMBL109631 — IC50 = 110.0 nM 6.96
CHEMBL448154 — IC50 = 110.0 nM 6.96
CHEMBL113070 — IC50 = 110.0 nM 6.96
CHEMBL325589 — IC50 = 150.0 nM 6.82
CHEMBL323405 — IC50 = 150.0 nM 6.82
CHEMBL321193 — IC50 = 180.0 nM 6.75
CHEMBL104779 — IC50 = 190.0 nM 6.72
CHEMBL322298 — IC50 = 210.0 nM 6.68
CHEMBL106232 — IC50 = 240.0 nM 6.62
CHEMBL104244 — IC50 = 320.0 nM 6.50
CHEMBL111197 — IC50 = 370.0 nM 6.43
CHEMBL299194 — IC50 = 380.0 nM 6.42
CHEMBL104153 — IC50 = 410.0 nM 6.39
CHEMBL324926 — IC50 = 430.0 nM 6.37
CHEMBL113023 — IC50 = 450.0 nM 6.35
CHEMBL301612 — IC50 = 460.0 nM 6.34
CHEMBL111365 — IC50 = 540.0 nM 6.27
CHEMBL113863 — IC50 = 580.0 nM 6.24
CHEMBL109759 — IC50 = 700.0 nM 6.16
CHEMBL111339 — IC50 = 910.0 nM 6.04
CHEMBL109296 — IC50 = 960.0 nM 6.02
CHEMBL49596 — IC50 = 1300.0 nM 5.89
CHEMBL48172 — IC50 = 1410.0 nM 5.85
CHEMBL109547 — IC50 = 1500.0 nM 5.82
CHEMBL111618 — IC50 = 1660.0 nM 5.78
CHEMBL111434 — IC50 = 2400.0 nM 5.62
CHEMBL107472 — IC50 = 2500.0 nM 5.60
CHEMBL419022 — IC50 = 2600.0 nM 5.58
CHEMBL111247 — IC50 = 3000.0 nM 5.52
CHEMBL320705 — IC50 = 3200.0 nM 5.50
CHEMBL110034 — IC50 = 3150.0 nM 5.50
CHEMBL326041 — IC50 = 3210.0 nM 5.49
CHEMBL332269 — IC50 = 4480.0 nM 5.35
CHEMBL111913 — IC50 = 5800.0 nM 5.24
CHEMBL323699 — IC50 = 6530.0 nM 5.18
CHEMBL113128 — IC50 = 6800.0 nM 5.17
CHEMBL50470 — IC50 = 13900.0 nM 4.86
CHEMBL113356 — IC50 = 14000.0 nM 4.85