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Assay Detail

CHEMBL4317002

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Functional
Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MM1.S
Confidence 1 — Organism
Curated By Autocuration

Target

MM1.S (CHEMBL4296471)
Type CELL-LINE
Organism Homo sapiens

Publication

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Wang X, Blackaby W, Allen V, Chan GKY, Chang JH, Chiang PC, Diène C, Drummond J, Do S, Fan E, Harstad EB, Hodges A, Hu H, Jia W, Kofie W, Kolesnikov A, Lyssikatos JP, Ly J, Matteucci M, Moffat JG, Munugalavadla V, Murray J, Nash D, Noland CL, Del Rosario G, Ross L, Rouse C, Sharpe A, Slaga D, Sun M, Tsui V, Wallweber H, Yu SF, Ebens AJ.
J Med Chem (2019) 62 : 2140 -2153
PubMed 30715878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.76 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4459538 1 8.10
CHEMBL4453890 1 7.52
CHEMBL3623150 1 7.40
CHEMBL3676285 1 7.30
CHEMBL3648724 1 7.30
CHEMBL4109141 1 7.16
CHEMBL4439756 1 7.16
CHEMBL3648680 1 7.16
CHEMBL4437940 1 7.10
CHEMBL3648675 1 7.00
CHEMBL521851 PICTILISIB 2.0 1 7.00
CHEMBL3103867 1 6.80
CHEMBL4469964 1 6.70
CHEMBL4450356 1 6.30
CHEMBL3623162 1 6.05
CHEMBL4472966 1 5.68
CHEMBL4455188 1 5.10
CHEMBL4458081 1 4.89
CHEMBL4449930 1 -
CHEMBL4449080 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4459538 IC50 = 8.0 nM 8.10
CHEMBL4453890 IC50 = 30.0 nM 7.52
CHEMBL3623150 IC50 = 40.0 nM 7.40
CHEMBL3676285 IC50 = 50.0 nM 7.30
CHEMBL3648724 IC50 = 50.0 nM 7.30
CHEMBL4109141 IC50 = 70.0 nM 7.16
CHEMBL4439756 IC50 = 70.0 nM 7.16
CHEMBL3648680 IC50 = 70.0 nM 7.16
CHEMBL4437940 IC50 = 80.0 nM 7.10
CHEMBL3648675 IC50 = 100.0 nM 7.00
CHEMBL521851 PICTILISIB IC50 = 100.0 nM 7.00
CHEMBL3103867 IC50 = 160.0 nM 6.80
CHEMBL4469964 IC50 = 200.0 nM 6.70
CHEMBL4450356 IC50 = 500.0 nM 6.30
CHEMBL3623162 IC50 = 900.0 nM 6.05
CHEMBL4472966 IC50 = 2100.0 nM 5.68
CHEMBL4455188 IC50 = 8000.0 nM 5.10
CHEMBL4458081 IC50 = 13000.0 nM 4.89
CHEMBL4449930 IC50 - -
CHEMBL4449080 IC50 > 25000.0 nM -