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Assay Detail

CHEMBL4270677

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

Functional
Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type K562
Confidence 1 — Organism
Curated By Intermediate

Target

K562 (CHEMBL385)
Type CELL-LINE
Organism Homo sapiens

Publication

ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles.
Řezníčková E, Tenora L, Pospíšilová P, Galeta J, Jorda R, Berka K, Majer P, Potáček M, Kryštof V.
Eur J Med Chem (2017) 127 : 632 -642
PubMed 28135685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 4.23 4.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4279172 1 4.62
CHEMBL4291675 1 4.51
CHEMBL4294411 1 4.35
CHEMBL4292491 1 4.28
CHEMBL4284266 1 4.19
CHEMBL4281195 1 4.13
CHEMBL4287261 1 4.11
CHEMBL4283308 1 4.11
CHEMBL4287412 1 4.09
CHEMBL4292170 1 4.06
CHEMBL4289487 1 4.04
CHEMBL4284434 1 -
CHEMBL4281030 1 -
CHEMBL4277021 1 -
CHEMBL4287654 1 -
CHEMBL4285400 1 -
CHEMBL4277446 1 -
CHEMBL4288745 1 -
CHEMBL4279331 1 -
CHEMBL4278812 1 -
CHEMBL4292878 1 -
CHEMBL4279935 1 -
CHEMBL185238 GW786460X 1 -
CHEMBL4291439 1 -
CHEMBL4284609 1 -
CHEMBL4276896 1 -
CHEMBL4285692 1 -
CHEMBL4277755 1 -
CHEMBL2364611 GALUNISERTIB 2.0 1 -
CHEMBL4282287 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4279172 IC50 = 24000.0 nM 4.62
CHEMBL4291675 IC50 = 31000.0 nM 4.51
CHEMBL4294411 IC50 = 45000.0 nM 4.35
CHEMBL4292491 IC50 = 52000.0 nM 4.28
CHEMBL4284266 IC50 = 64000.0 nM 4.19
CHEMBL4281195 IC50 = 74000.0 nM 4.13
CHEMBL4287261 IC50 = 77000.0 nM 4.11
CHEMBL4283308 IC50 = 77000.0 nM 4.11
CHEMBL4287412 IC50 = 82000.0 nM 4.09
CHEMBL4292170 IC50 = 88000.0 nM 4.06
CHEMBL4289487 IC50 = 92000.0 nM 4.04
CHEMBL4287843 IC50 > 100000.0 nM -
CHEMBL4284434 IC50 > 100000.0 nM -
CHEMBL4281030 IC50 > 100000.0 nM -
CHEMBL4277021 IC50 > 100000.0 nM -
CHEMBL4287654 IC50 > 100000.0 nM -
CHEMBL4285400 IC50 > 100000.0 nM -
CHEMBL4277446 IC50 > 50000.0 nM -
CHEMBL4288745 IC50 > 100000.0 nM -
CHEMBL4279331 IC50 > 12000.0 nM -
CHEMBL4278812 IC50 > 12000.0 nM -
CHEMBL4292878 IC50 > 100000.0 nM -
CHEMBL4279935 IC50 > 100000.0 nM -
CHEMBL185238 GW786460X IC50 > 100000.0 nM -
CHEMBL4291439 IC50 > 25000.0 nM -
CHEMBL4284609 IC50 > 100000.0 nM -
CHEMBL4276896 IC50 > 100000.0 nM -
CHEMBL4285692 IC50 > 100000.0 nM -
CHEMBL4277755 IC50 > 100000.0 nM -
CHEMBL2364611 GALUNISERTIB IC50 - -
CHEMBL4282287 IC50 > 100000.0 nM -