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Assay Detail

CHEMBL666089

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

Binding
Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring the phosphorylation of RbING
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601)
Type PROTEIN COMPLEX
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 15 6.50 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332575 1 7.35
CHEMBL388978 STAUROSPORINE 1 7.23
CHEMBL268368 STAUROSPORINE AGLYCON 1 6.85
CHEMBL127532 1 6.82
CHEMBL340685 1 6.75
CHEMBL126545 1 6.66
CHEMBL338264 1 6.60
CHEMBL421087 1 6.58
CHEMBL125627 1 6.39
CHEMBL338289 1 6.37
CHEMBL240747 GRANULATIMIDE 1 6.13
CHEMBL16958 STAUROSPORINONE 1 6.08
CHEMBL126447 1 5.74
CHEMBL127277 1 5.42
CHEMBL341503 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332575 IC50 = 45.0 nM 7.35
CHEMBL388978 STAUROSPORINE IC50 = 59.0 nM 7.23
CHEMBL268368 STAUROSPORINE AGLYCON IC50 = 140.0 nM 6.85
CHEMBL127532 IC50 = 150.0 nM 6.82
CHEMBL340685 IC50 = 180.0 nM 6.75
CHEMBL126545 IC50 = 220.0 nM 6.66
CHEMBL338264 IC50 = 250.0 nM 6.60
CHEMBL421087 IC50 = 260.0 nM 6.58
CHEMBL125627 IC50 = 410.0 nM 6.39
CHEMBL338289 IC50 = 430.0 nM 6.37
CHEMBL240747 GRANULATIMIDE IC50 = 740.0 nM 6.13
CHEMBL16958 STAUROSPORINONE IC50 = 830.0 nM 6.08
CHEMBL126447 IC50 = 1810.0 nM 5.74
CHEMBL127277 IC50 = 3830.0 nM 5.42
CHEMBL341503 IC50 > 10000.0 nM -