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Assay Detail

CHEMBL770469

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

Binding
Inhibition of phosphorylation of a random glutamate/tyrosine copolymer in lysates of transfected Sf9 insect cells overexpressing mouse platelet-derived growth factor receptor beta
ChEMBL ↗
92
Total Activities
92
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor.
Palmer BD, Smaill JB, Boyd M, Boschelli DH, Doherty AM, Hamby JM, Khatana SS, Kramer JB, Kraker AJ, Panek RL, Lu GH, Dahring TK, Winters RT, Showalter HD, Denny WA.
J Med Chem (1998) 41 : 5457 -5465
PubMed 9876115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 92 5.04 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76202 — — 1 6.37
CHEMBL80873 — — 1 6.36
CHEMBL358469 — — 1 6.16
CHEMBL153054 — — 1 6.08
CHEMBL150568 — — 1 6.07
CHEMBL348242 — — 1 5.75
CHEMBL153106 — — 1 5.68
CHEMBL153084 — — 1 5.60
CHEMBL150973 — — 1 5.57
CHEMBL155505 — — 1 5.44
CHEMBL348706 — — 1 5.42
CHEMBL436455 — — 1 5.40
CHEMBL152934 — — 1 5.36
CHEMBL153328 — — 1 5.27
CHEMBL346870 — — 1 5.25
CHEMBL356169 — — 1 5.19
CHEMBL151956 — — 1 5.17
CHEMBL434312 — — 1 5.14
CHEMBL358384 — — 1 5.08
CHEMBL150504 — — 1 5.03
CHEMBL310080 — — 1 5.03
CHEMBL450929 — — 1 5.00
CHEMBL75964 — — 1 4.96
CHEMBL358429 — — 1 4.92
CHEMBL153512 — — 1 4.89
CHEMBL153101 — — 1 4.89
CHEMBL359055 — — 1 4.89
CHEMBL356237 — — 1 4.80
CHEMBL358446 — — 1 4.80
CHEMBL153208 — — 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76202 — IC50 = 430.0 nM 6.37
CHEMBL80873 — IC50 = 440.0 nM 6.36
CHEMBL358469 — IC50 = 700.0 nM 6.16
CHEMBL153054 — IC50 = 830.0 nM 6.08
CHEMBL150568 — IC50 = 860.0 nM 6.07
CHEMBL348242 — IC50 = 1800.0 nM 5.75
CHEMBL153106 — IC50 = 2100.0 nM 5.68
CHEMBL153084 — IC50 = 2500.0 nM 5.60
CHEMBL150973 — IC50 = 2700.0 nM 5.57
CHEMBL155505 — IC50 = 3600.0 nM 5.44
CHEMBL348706 — IC50 = 3800.0 nM 5.42
CHEMBL436455 — IC50 = 4000.0 nM 5.40
CHEMBL152934 — IC50 = 4400.0 nM 5.36
CHEMBL153328 — IC50 = 5400.0 nM 5.27
CHEMBL346870 — IC50 = 5600.0 nM 5.25
CHEMBL356169 — IC50 = 6400.0 nM 5.19
CHEMBL151956 — IC50 = 6800.0 nM 5.17
CHEMBL434312 — IC50 = 7200.0 nM 5.14
CHEMBL358384 — IC50 = 8400.0 nM 5.08
CHEMBL150504 — IC50 = 9300.0 nM 5.03
CHEMBL310080 — IC50 = 9300.0 nM 5.03
CHEMBL450929 — IC50 = 10000.0 nM 5.00
CHEMBL75964 — IC50 = 11000.0 nM 4.96
CHEMBL358429 — IC50 = 12000.0 nM 4.92
CHEMBL359055 — IC50 = 13000.0 nM 4.89
CHEMBL153101 — IC50 = 13000.0 nM 4.89
CHEMBL153512 — IC50 = 13000.0 nM 4.89
CHEMBL356237 — IC50 = 16000.0 nM 4.80
CHEMBL358446 — IC50 = 16000.0 nM 4.80
CHEMBL153208 — IC50 = 16000.0 nM 4.80
CHEMBL435677 — IC50 = 16000.0 nM 4.80
CHEMBL155093 — IC50 = 19000.0 nM 4.72
CHEMBL152995 — IC50 = 23000.0 nM 4.64
CHEMBL345730 — IC50 = 23000.0 nM 4.64
CHEMBL153682 — IC50 = 24000.0 nM 4.62
CHEMBL346611 — IC50 = 25000.0 nM 4.60
CHEMBL356679 — IC50 = 25000.0 nM 4.60
CHEMBL153110 — IC50 = 28000.0 nM 4.55
CHEMBL346000 — IC50 = 28000.0 nM 4.55
CHEMBL345970 — IC50 = 30000.0 nM 4.52
CHEMBL153526 — IC50 = 37000.0 nM 4.43
CHEMBL347777 — IC50 = 40000.0 nM 4.40
CHEMBL150573 — IC50 = 47000.0 nM 4.33
CHEMBL153624 — IC50 = 50000.0 nM 4.30
CHEMBL149401 — IC50 = 50000.0 nM 4.30
CHEMBL149458 — IC50 = 50000.0 nM 4.30
CHEMBL358243 — IC50 = 50000.0 nM 4.30
CHEMBL154978 — IC50 > 50000.0 nM -
CHEMBL150575 — IC50 > 50000.0 nM -
CHEMBL153477 — IC50 > 50000.0 nM -