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Assay Detail

CHEMBL3824534

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

Functional
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 days by PrestoBlue assay
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 1 — Organism
Curated By Autocuration

Target

MDA-MB-231 (CHEMBL400)
Type CELL-LINE
Organism Homo sapiens

Publication

Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.
Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC, Brunton VG, Patton EE, Carragher NO, Unciti-Broceta A.
J Med Chem (2016) 59 : 4697 -4710
PubMed 27115835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 5.67 8.05
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3824089 1 8.05
CHEMBL3824116 1 7.51
CHEMBL3824233 1 7.41
CHEMBL3823620 1 7.14
CHEMBL3823104 1 7.09
CHEMBL3823543 1 6.78
CHEMBL3824279 1 5.71
CHEMBL3823506 1 5.70
CHEMBL3823451 1 5.56
CHEMBL3824228 1 5.45
CHEMBL3823845 1 5.38
CHEMBL3823948 1 5.38
CHEMBL3822874 1 5.17
CHEMBL3822579 1 5.01
CHEMBL3823239 1 4.91
CHEMBL3823255 1 4.87
CHEMBL3823711 1 4.82
CHEMBL3823108 1 4.75
CHEMBL3822469 1 4.57
CHEMBL3822652 1 4.54
CHEMBL3823660 1 4.49
CHEMBL3823135 1 4.40
CHEMBL3823861 1 -
CHEMBL3824021 1 -
CHEMBL3824156 1 -
CHEMBL3823344 1 -
CHEMBL1241481 1 -
CHEMBL5416410 DASATINIB 4.0 1 -
CHEMBL3823556 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3824089 EC50 = 9.0 nM 8.05
CHEMBL3824116 EC50 = 31.0 nM 7.51
CHEMBL3824233 EC50 = 39.0 nM 7.41
CHEMBL3823620 EC50 = 73.0 nM 7.14
CHEMBL3823104 EC50 = 81.0 nM 7.09
CHEMBL3823543 EC50 = 167.0 nM 6.78
CHEMBL3824279 EC50 = 1960.0 nM 5.71
CHEMBL3823506 EC50 = 1990.0 nM 5.70
CHEMBL3823451 EC50 = 2760.0 nM 5.56
CHEMBL3824228 EC50 = 3570.0 nM 5.45
CHEMBL3823845 EC50 = 4140.0 nM 5.38
CHEMBL3823948 EC50 = 4150.0 nM 5.38
CHEMBL3822874 EC50 = 6720.0 nM 5.17
CHEMBL3822579 EC50 = 9710.0 nM 5.01
CHEMBL3823239 EC50 = 12180.0 nM 4.91
CHEMBL3823255 EC50 = 13590.0 nM 4.87
CHEMBL3823711 EC50 = 15230.0 nM 4.82
CHEMBL3823108 EC50 = 17740.0 nM 4.75
CHEMBL3822469 EC50 = 26770.0 nM 4.57
CHEMBL3822652 EC50 = 28590.0 nM 4.54
CHEMBL3823660 EC50 = 32600.0 nM 4.49
CHEMBL3823135 EC50 = 40200.0 nM 4.40
CHEMBL3823861 Activity - -
CHEMBL3824021 EC50 > 100000.0 nM -
CHEMBL3824156 EC50 > 100000.0 nM -
CHEMBL3823344 EC50 > 100000.0 nM -
CHEMBL1241481 Activity - -
CHEMBL5416410 DASATINIB Activity - -
CHEMBL3823556 Activity - -