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Assay Detail

CHEMBL5529675

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

Binding
Inhibition of ATM in human HT-29 cells incubated for 2 hrs by Alexa Fluor 488/Hoeschst staining based plate reader assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine-protein kinase ATM (CHEMBL3797)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
Pike KG, Hunt TA, Barlaam B, Benstead D, Cadogan E, Chen K, Cook CR, Colclough N, Deng C, Durant ST, Eatherton A, Goldberg K, Johnström P, Liu L, Liu Z, Nissink JWM, Pang C, Pass M, Robb GR, Roberts C, Schou M, Steward O, Sykes A, Yan Y, Zhai B, Zheng L.
J Med Chem (2024) 67 : 3090 -3111
PubMed 38306388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.36 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5573231 1 9.90
CHEMBL5572255 1 9.60
CHEMBL5567522 1 9.60
CHEMBL5171429 1 9.60
CHEMBL5182423 1 9.40
CHEMBL5571791 1 9.30
CHEMBL5573212 1 9.30
CHEMBL3960662 1 9.20
CHEMBL5595653 1 9.10
CHEMBL4594429 AZD-1390 1.0 1 9.10
CHEMBL5565468 1 9.00
CHEMBL5555756 1 9.00
CHEMBL5566946 1 8.80
CHEMBL5583538 1 8.70
CHEMBL5575507 1 8.70
CHEMBL5567347 1 8.50
CHEMBL5569887 1 8.20
CHEMBL5575600 1 8.20
CHEMBL5571248 1 8.00
CHEMBL5571179 1 7.90
CHEMBL5570730 1 7.90
CHEMBL5566892 1 7.90
CHEMBL5569852 1 7.90
CHEMBL5590607 1 7.40
CHEMBL5563436 1 7.40
CHEMBL5567014 1 7.40
CHEMBL5573686 1 7.40
CHEMBL5532085 1 7.30
CHEMBL5178407 1 6.51
CHEMBL4169828 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5573231 IC50 = 0.1259 nM 9.90
CHEMBL5572255 IC50 = 0.2512 nM 9.60
CHEMBL5567522 IC50 = 0.2512 nM 9.60
CHEMBL5171429 IC50 = 0.2512 nM 9.60
CHEMBL5182423 IC50 = 0.3981 nM 9.40
CHEMBL5571791 IC50 = 0.5012 nM 9.30
CHEMBL5573212 IC50 = 0.5012 nM 9.30
CHEMBL3960662 IC50 = 0.631 nM 9.20
CHEMBL5595653 IC50 = 0.7943 nM 9.10
CHEMBL4594429 AZD-1390 IC50 = 0.7943 nM 9.10
CHEMBL5565468 IC50 = 1.0 nM 9.00
CHEMBL5555756 IC50 = 1.0 nM 9.00
CHEMBL5566946 IC50 = 1.585 nM 8.80
CHEMBL5583538 IC50 = 1.995 nM 8.70
CHEMBL5575507 IC50 = 1.995 nM 8.70
CHEMBL5567347 IC50 = 3.162 nM 8.50
CHEMBL5569887 IC50 = 6.31 nM 8.20
CHEMBL5575600 IC50 = 6.31 nM 8.20
CHEMBL5571248 IC50 = 10.0 nM 8.00
CHEMBL5571179 IC50 = 12.59 nM 7.90
CHEMBL5570730 IC50 = 12.59 nM 7.90
CHEMBL5566892 IC50 = 12.59 nM 7.90
CHEMBL5569852 IC50 = 12.59 nM 7.90
CHEMBL5590607 IC50 = 39.81 nM 7.40
CHEMBL5563436 IC50 = 39.81 nM 7.40
CHEMBL5567014 IC50 = 39.81 nM 7.40
CHEMBL5573686 IC50 = 39.81 nM 7.40
CHEMBL5532085 IC50 = 50.12 nM 7.30
CHEMBL5178407 IC50 = 310.0 nM 6.51
CHEMBL4169828 IC50 = 316.23 nM 6.50
CHEMBL4167508 IC50 = 398.11 nM 6.40