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Assay Detail

CHEMBL764165

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Binding
Inhibitory concentration was evaluated against Platelet-derived growth factor receptor beta (PDGFr) tyrosine kinase
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Platelet-derived growth factor receptor beta (CHEMBL2749) ↗
Type SINGLE PROTEIN
Organism Mus musculus

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 56 6.09 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50647 — — 1 7.14
CHEMBL331366 — — 1 7.13
CHEMBL49120 PD-0166285 1.0 1 7.10
CHEMBL324543 — — 1 7.09
CHEMBL112080 — — 1 7.02
CHEMBL323775 — — 1 7.01
CHEMBL448154 — — 1 7.00
CHEMBL112706 — — 1 7.00
CHEMBL104779 — — 1 7.00
CHEMBL297523 — — 1 6.99
CHEMBL51283 — — 1 6.96
CHEMBL325589 — — 1 6.92
CHEMBL320339 — — 1 6.92
CHEMBL110905 — — 1 6.92
CHEMBL113070 — — 1 6.92
CHEMBL109631 — — 1 6.89
CHEMBL112914 — — 1 6.82
CHEMBL113521 — — 1 6.72
CHEMBL327127 — — 1 6.68
CHEMBL323405 — — 1 6.55
CHEMBL301612 — — 1 6.40
CHEMBL111365 — — 1 6.40
CHEMBL321193 — — 1 6.39
CHEMBL111197 — — 1 6.28
CHEMBL104153 — — 1 6.17
CHEMBL106232 — — 1 6.15
CHEMBL113863 — — 1 6.14
CHEMBL322298 — — 1 6.10
CHEMBL104244 — — 1 6.05
CHEMBL111339 — — 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50647 — IC50 = 72.0 nM 7.14
CHEMBL331366 — IC50 = 74.0 nM 7.13
CHEMBL49120 PD-0166285 IC50 = 79.0 nM 7.10
CHEMBL324543 — IC50 = 81.0 nM 7.09
CHEMBL112080 — IC50 = 96.0 nM 7.02
CHEMBL323775 — IC50 = 98.0 nM 7.01
CHEMBL448154 — IC50 = 100.0 nM 7.00
CHEMBL112706 — IC50 = 101.0 nM 7.00
CHEMBL104779 — IC50 = 100.0 nM 7.00
CHEMBL297523 — IC50 = 103.0 nM 6.99
CHEMBL51283 — IC50 = 110.0 nM 6.96
CHEMBL113070 — IC50 = 120.0 nM 6.92
CHEMBL110905 — IC50 = 120.0 nM 6.92
CHEMBL320339 — IC50 = 120.0 nM 6.92
CHEMBL325589 — IC50 = 120.0 nM 6.92
CHEMBL109631 — IC50 = 130.0 nM 6.89
CHEMBL112914 — IC50 = 150.0 nM 6.82
CHEMBL113521 — IC50 = 190.0 nM 6.72
CHEMBL327127 — IC50 = 210.0 nM 6.68
CHEMBL323405 — IC50 = 280.0 nM 6.55
CHEMBL301612 — IC50 = 400.0 nM 6.40
CHEMBL111365 — IC50 = 400.0 nM 6.40
CHEMBL321193 — IC50 = 410.0 nM 6.39
CHEMBL111197 — IC50 = 530.0 nM 6.28
CHEMBL104153 — IC50 = 680.0 nM 6.17
CHEMBL106232 — IC50 = 710.0 nM 6.15
CHEMBL113863 — IC50 = 730.0 nM 6.14
CHEMBL322298 — IC50 = 800.0 nM 6.10
CHEMBL104244 — IC50 = 890.0 nM 6.05
CHEMBL111339 — IC50 = 1200.0 nM 5.92
CHEMBL113023 — IC50 = 1500.0 nM 5.82
CHEMBL109547 — IC50 = 1700.0 nM 5.77
CHEMBL324926 — IC50 = 1700.0 nM 5.77
CHEMBL320705 — IC50 = 1800.0 nM 5.75
CHEMBL111247 — IC50 = 2600.0 nM 5.58
CHEMBL299194 — IC50 = 2800.0 nM 5.55
CHEMBL111434 — IC50 = 3100.0 nM 5.51
CHEMBL109759 — IC50 = 3200.0 nM 5.50
CHEMBL109296 — IC50 = 4000.0 nM 5.40
CHEMBL419022 — IC50 = 4200.0 nM 5.38
CHEMBL326041 — IC50 = 4800.0 nM 5.32
CHEMBL49596 — IC50 = 4900.0 nM 5.31
CHEMBL111913 — IC50 = 5200.0 nM 5.28
CHEMBL107472 — IC50 = 6200.0 nM 5.21
CHEMBL111618 — IC50 = 6500.0 nM 5.19
CHEMBL110034 — IC50 = 6600.0 nM 5.18
CHEMBL48172 — IC50 = 6800.0 nM 5.17
CHEMBL50470 — IC50 = 8900.0 nM 5.05
CHEMBL323699 — IC50 = 9300.0 nM 5.03
CHEMBL332269 — IC50 = 10300.0 nM 4.99