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Assay Detail

CHEMBL4194885

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

Functional
Antiproliferative activity against human MX1 cells incubated for 72 hrs by cell-titer Glo assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MX1
Confidence 1 — Organism
Curated By Intermediate

Target

MX1 (CHEMBL613704)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Fidanze SD, Liu D, Mantei RA, Hasvold LA, Pratt JK, Sheppard GS, Wang L, Holms JH, Dai Y, Aguirre A, Bogdan A, Dietrich JD, Marjanovic J, Park CH, Hutchins CW, Lin X, Bui MH, Huang X, Wilcox D, Li L, Wang R, Kovar P, Magoc TJ, Rajaraman G, Albert DH, Shen Y, Kati WM, McDaniel KF.
Bioorg Med Chem Lett (2018) 28 : 1804 -1810
PubMed 29678460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 7.83 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4212498 1 9.14
CHEMBL4208129 1 8.89
CHEMBL4215988 1 8.85
CHEMBL4208136 1 8.85
CHEMBL4212062 1 8.70
CHEMBL4217457 1 8.47
CHEMBL4204316 1 8.40
CHEMBL4217818 1 8.33
CHEMBL4214501 1 8.31
CHEMBL4213481 1 8.26
CHEMBL4218411 1 8.25
CHEMBL4213045 1 8.15
CHEMBL4215043 1 8.14
CHEMBL4202833 1 8.11
CHEMBL3987016 MIVEBRESIB 2.0 1 7.89
CHEMBL4202497 1 7.82
CHEMBL4203764 1 7.80
CHEMBL3978817 1 7.77
CHEMBL4206058 1 7.75
CHEMBL4210131 1 7.72
CHEMBL3903195 1 7.37
CHEMBL4217560 1 7.24
CHEMBL4208643 1 7.11
CHEMBL4215025 1 6.85
CHEMBL4207179 1 6.85
CHEMBL4207708 1 6.85
CHEMBL3904546 1 5.85
CHEMBL4203377 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4212498 EC50 = 0.72 nM 9.14
CHEMBL4208129 EC50 = 1.3 nM 8.89
CHEMBL4215988 EC50 = 1.4 nM 8.85
CHEMBL4208136 EC50 = 1.4 nM 8.85
CHEMBL4212062 EC50 = 2.0 nM 8.70
CHEMBL4217457 EC50 = 3.4 nM 8.47
CHEMBL4204316 EC50 = 4.0 nM 8.40
CHEMBL4217818 EC50 = 4.7 nM 8.33
CHEMBL4214501 EC50 = 4.9 nM 8.31
CHEMBL4213481 EC50 = 5.5 nM 8.26
CHEMBL4218411 EC50 = 5.6 nM 8.25
CHEMBL4213045 EC50 = 7.0 nM 8.15
CHEMBL4215043 EC50 = 7.3 nM 8.14
CHEMBL4202833 EC50 = 7.8 nM 8.11
CHEMBL3987016 MIVEBRESIB EC50 = 13.0 nM 7.89
CHEMBL4202497 EC50 = 15.0 nM 7.82
CHEMBL4203764 EC50 = 16.0 nM 7.80
CHEMBL3978817 EC50 = 17.0 nM 7.77
CHEMBL4206058 EC50 = 18.0 nM 7.75
CHEMBL4210131 EC50 = 19.0 nM 7.72
CHEMBL3903195 EC50 = 43.0 nM 7.37
CHEMBL4217560 EC50 = 57.0 nM 7.24
CHEMBL4208643 EC50 = 78.0 nM 7.11
CHEMBL4215025 EC50 = 140.0 nM 6.85
CHEMBL4207179 EC50 = 140.0 nM 6.85
CHEMBL4207708 EC50 = 140.0 nM 6.85
CHEMBL3904546 EC50 = 1400.0 nM 5.85
CHEMBL4203377 EC50 = 3300.0 nM 5.48