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Assay Detail

CHEMBL5349013

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Functional
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MOLM-13
Confidence 1 — Organism
Curated By Autocuration

Target

MOLM-13 (CHEMBL3706572)
Type CELL-LINE
Organism Homo sapiens

Publication

From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors.
Koravovic M, Mayasundari A, Tasic G, Keramatnia F, Stachowski TR, Cui H, Chai SC, Jonchere B, Yang L, Li Y, Fu X, Hiltenbrand R, Paul L, Mishra V, Klco JM, Roussel MF, Pomerantz WC, Fischer M, Rankovic Z, Savic V.
Eur J Med Chem (2023) 251 : 115246 -115246
PubMed 36898329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.57 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5440963 1 8.70
CHEMBL5422163 1 8.52
CHEMBL5436475 1 8.10
CHEMBL5400310 1 8.10
CHEMBL5424952 1 8.05
CHEMBL5432745 1 8.00
CHEMBL3581647 BIRABRESIB 2.0 1 7.96
CHEMBL5420752 1 7.96
CHEMBL5440537 1 7.85
CHEMBL5439607 1 7.66
CHEMBL1957266 1 7.62
CHEMBL5403848 1 7.28
CHEMBL5399489 1 6.70
CHEMBL5398000 1 6.50
CHEMBL5401253 1 6.42
CHEMBL5422881 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5440963 IC50 = 2.0 nM 8.70
CHEMBL5422163 IC50 = 3.0 nM 8.52
CHEMBL5436475 IC50 = 8.0 nM 8.10
CHEMBL5400310 IC50 = 8.0 nM 8.10
CHEMBL5424952 IC50 = 9.0 nM 8.05
CHEMBL5432745 IC50 = 10.0 nM 8.00
CHEMBL3581647 BIRABRESIB IC50 = 11.0 nM 7.96
CHEMBL5420752 IC50 = 11.0 nM 7.96
CHEMBL5440537 IC50 = 14.0 nM 7.85
CHEMBL5439607 IC50 = 22.0 nM 7.66
CHEMBL1957266 IC50 = 24.0 nM 7.62
CHEMBL5403848 IC50 = 52.0 nM 7.28
CHEMBL5399489 IC50 = 200.0 nM 6.70
CHEMBL5398000 IC50 = 318.0 nM 6.50
CHEMBL5401253 IC50 = 385.0 nM 6.42
CHEMBL5422881 IC50 = 2402.0 nM 5.62