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Assay Detail

CHEMBL4845014

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

Functional
Antiproliferative activity against mouse NFS-60 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NFS-60
Confidence 1 — Organism
Curated By Autocuration

Target

NFS-60 (CHEMBL614199)
Type CELL-LINE
Organism Mus musculus

Publication

Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model.
Lee KH, Yen WC, Lin WH, Wang PC, Lai YL, Su YC, Chang CY, Wu CS, Huang YC, Yang CM, Chou LH, Yeh TK, Chen CT, Shih C, Hsieh HP.
J Med Chem (2021) 64 : 14477 -14497
PubMed 34606263 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 7.03 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4846051 1 7.64
CHEMBL4877440 1 7.64
CHEMBL4846414 1 7.60
CHEMBL4877148 1 7.28
CHEMBL4860468 1 7.26
CHEMBL4873828 1 7.24
CHEMBL4870360 1 7.17
CHEMBL4846384 1 7.17
CHEMBL4851635 1 7.16
CHEMBL1908396 1 7.11
CHEMBL4870448 1 7.09
CHEMBL4877247 1 7.04
CHEMBL4847875 1 7.02
CHEMBL4854210 1 7.01
CHEMBL4857271 1 6.97
CHEMBL4859405 1 6.85
CHEMBL4857617 1 6.84
CHEMBL4864248 1 6.84
CHEMBL4878471 1 6.82
CHEMBL4849425 1 6.79
CHEMBL4863584 1 6.70
CHEMBL3813873 PEXIDARTINIB 4.0 1 6.53
CHEMBL4857690 1 5.96
CHEMBL4866196 1 -
CHEMBL4878293 1 -
CHEMBL4851545 1 -
CHEMBL4876396 1 -
CHEMBL4878431 1 -
CHEMBL4874053 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4846051 EC50 = 23.0 nM 7.64
CHEMBL4877440 EC50 = 23.0 nM 7.64
CHEMBL4846414 EC50 = 25.0 nM 7.60
CHEMBL4877148 EC50 = 53.0 nM 7.28
CHEMBL4860468 EC50 = 55.0 nM 7.26
CHEMBL4873828 EC50 = 58.0 nM 7.24
CHEMBL4870360 EC50 = 67.0 nM 7.17
CHEMBL4846384 EC50 = 68.0 nM 7.17
CHEMBL4851635 EC50 = 69.0 nM 7.16
CHEMBL1908396 EC50 = 77.0 nM 7.11
CHEMBL4870448 EC50 = 81.0 nM 7.09
CHEMBL4877247 EC50 = 92.0 nM 7.04
CHEMBL4847875 EC50 = 95.0 nM 7.02
CHEMBL4854210 EC50 = 97.0 nM 7.01
CHEMBL4857271 EC50 = 108.0 nM 6.97
CHEMBL4859405 EC50 = 141.0 nM 6.85
CHEMBL4857617 EC50 = 144.0 nM 6.84
CHEMBL4864248 EC50 = 145.0 nM 6.84
CHEMBL4878471 EC50 = 152.0 nM 6.82
CHEMBL4849425 EC50 = 162.0 nM 6.79
CHEMBL4863584 EC50 = 202.0 nM 6.70
CHEMBL3813873 PEXIDARTINIB EC50 = 294.0 nM 6.53
CHEMBL4857690 EC50 = 1090.0 nM 5.96
CHEMBL4866196 EC50 - -
CHEMBL4878293 EC50 - -
CHEMBL4851545 EC50 - -
CHEMBL4876396 EC50 - -
CHEMBL4878431 EC50 - -
CHEMBL4874053 EC50 - -