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Assay Detail

CHEMBL751336

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

Functional
Inhibition of human NCI-H460 (lung) carcinoma cell proliferation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H460
Confidence 1 — Organism
Curated By Expert

Target

NCI-H460 (CHEMBL396)
Type CELL-LINE
Organism Homo sapiens

Publication

Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.
Sanchez-Martinez C, Shih C, Faul MM, Zhu G, Paal M, Somoza C, Li T, Kumrich CA, Winneroski LL, Xun Z, Brooks HB, Patel BK, Schultz RM, DeHahn TB, Spencer CD, Watkins SA, Considine E, Dempsey JA, Ogg CA, Campbell RM, Anderson BA, Wagner J.
Bioorg Med Chem Lett (2003) 13 : 3835 -3839
PubMed 14552791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.73 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268368 STAUROSPORINE AGLYCON 1 6.23
CHEMBL338264 1 5.94
CHEMBL332575 1 5.68
CHEMBL126545 1 5.55
CHEMBL16958 STAUROSPORINONE 1 5.50
CHEMBL421087 1 5.47
CHEMBL127532 1 -
CHEMBL338289 1 -
CHEMBL340685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 590.0 nM 6.23
CHEMBL338264 IC50 = 1160.0 nM 5.94
CHEMBL332575 IC50 = 2110.0 nM 5.68
CHEMBL126545 IC50 = 2840.0 nM 5.55
CHEMBL16958 STAUROSPORINONE IC50 = 3200.0 nM 5.50
CHEMBL421087 IC50 = 3420.0 nM 5.47
CHEMBL127532 IC50 > 10000.0 nM -
CHEMBL338289 IC50 > 10000.0 nM -
CHEMBL340685 IC50 > 10000.0 nM -