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Assay Detail

CHEMBL933669

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

Binding
Inhibition of FMS
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 Autocuration

Target

Macrophage colony-stimulating factor 1 receptor (CHEMBL1844)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based optimization of a potent class of arylamide FMS inhibitors.
Meegalla SK, Wall MJ, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Illig CR.
Bioorg Med Chem Lett (2008) 18 : 3632 -3637
PubMed 18495479 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.93 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL438533 1 9.52
CHEMBL402337 1 9.40
CHEMBL254702 1 9.10
CHEMBL257620 1 9.10
CHEMBL255443 1 9.10
CHEMBL257154 1 9.00
CHEMBL252436 1 9.00
CHEMBL256712 1 8.70
CHEMBL261699 1 8.70
CHEMBL402908 1 8.30
CHEMBL256950 1 8.10
CHEMBL258709 1 8.00
CHEMBL255501 1 7.82
CHEMBL430214 1 7.80
CHEMBL265432 1 7.75
CHEMBL411471 1 7.42
CHEMBL408431 1 7.27
CHEMBL257153 1 7.22
CHEMBL427775 1 7.22
CHEMBL429855 1 7.22
CHEMBL258461 1 6.33
CHEMBL258474 1 6.20
CHEMBL258680 1 6.05
CHEMBL265433 1 6.03
CHEMBL258238 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL438533 IC50 = 0.3 nM 9.52
CHEMBL402337 IC50 = 0.4 nM 9.40
CHEMBL254702 IC50 = 0.8 nM 9.10
CHEMBL257620 IC50 = 0.8 nM 9.10
CHEMBL255443 IC50 = 0.8 nM 9.10
CHEMBL257154 IC50 = 1.0 nM 9.00
CHEMBL252436 IC50 = 1.0 nM 9.00
CHEMBL256712 IC50 = 2.0 nM 8.70
CHEMBL261699 IC50 = 2.0 nM 8.70
CHEMBL402908 IC50 = 5.0 nM 8.30
CHEMBL256950 IC50 = 8.0 nM 8.10
CHEMBL258709 IC50 = 10.0 nM 8.00
CHEMBL255501 IC50 = 15.0 nM 7.82
CHEMBL430214 IC50 = 16.0 nM 7.80
CHEMBL265432 IC50 = 18.0 nM 7.75
CHEMBL411471 IC50 = 38.0 nM 7.42
CHEMBL408431 IC50 = 54.0 nM 7.27
CHEMBL257153 IC50 = 60.0 nM 7.22
CHEMBL427775 IC50 = 60.0 nM 7.22
CHEMBL429855 IC50 = 60.0 nM 7.22
CHEMBL258461 IC50 = 470.0 nM 6.33
CHEMBL258474 IC50 = 630.0 nM 6.20
CHEMBL258680 IC50 = 890.0 nM 6.05
CHEMBL265433 IC50 = 940.0 nM 6.03
CHEMBL258238 IC50 > 150.0 nM -