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Assay Detail

CHEMBL971707

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Functional
Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by alamar blue assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.
Wyatt PG, Woodhead AJ, Berdini V, Boulstridge JA, Carr MG, Cross DM, Davis DJ, Devine LA, Early TR, Feltell RE, Lewis EJ, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Reule M, Saxty G, Seavers LC, Smith DM, Squires MS, Trewartha G, Walker MT, Woolford AJ.
J Med Chem (2008) 51 : 4986 -4999
PubMed 18656911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.23 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497306 1 7.28
CHEMBL497477 1 7.20
CHEMBL445813 AT-7519 2.0 1 7.09
CHEMBL498659 1 6.89
CHEMBL507167 1 6.60
CHEMBL457388 1 6.51
CHEMBL457177 1 6.50
CHEMBL456963 1 6.26
CHEMBL448316 1 6.04
CHEMBL518383 1 5.85
CHEMBL510578 1 5.68
CHEMBL463579 1 5.47
CHEMBL463580 1 5.41
CHEMBL443198 1 4.48
CHEMBL457208 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497306 IC50 = 52.0 nM 7.28
CHEMBL497477 IC50 = 63.0 nM 7.20
CHEMBL445813 AT-7519 IC50 = 82.0 nM 7.09
CHEMBL498659 IC50 = 130.0 nM 6.89
CHEMBL507167 IC50 = 250.0 nM 6.60
CHEMBL457388 IC50 = 310.0 nM 6.51
CHEMBL457177 IC50 = 320.0 nM 6.50
CHEMBL456963 IC50 = 550.0 nM 6.26
CHEMBL448316 IC50 = 910.0 nM 6.04
CHEMBL518383 IC50 = 1400.0 nM 5.85
CHEMBL510578 IC50 = 2100.0 nM 5.68
CHEMBL463579 IC50 = 3400.0 nM 5.47
CHEMBL463580 IC50 = 3900.0 nM 5.41
CHEMBL443198 IC50 = 33000.0 nM 4.48
CHEMBL457208 IC50 - -