Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4668685

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

Binding
Inhibition of human CD73 expressed in CHO cells using AMP as substrate preincubated for 60 mins followed by substrate addition and measured after 60 mins by PiColorLock gold reagent based colorimetric assay
ChEMBL ↗
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5'-nucleotidase (CHEMBL5957) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of AB680: A Potent and Selective Inhibitor of CD73.
Lawson KV,Kalisiak J,Lindsey EA,Newcomb ET,Leleti MR,Debien L,Rosen BR,Miles DH,Sharif EU,Jeffrey JL,Tan JBL,Chen A,Zhao S,Xu G,Fu L,Jin L,Park TW,Berry W,Moschütz S,Scaletti E,Sträter N,Walker NP,Young SW,Walters MJ,Schindler U,Powers JP
J Med Chem (2020) 63 : 11448 -11468
PubMed 32614585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 9.00 10.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4749428 — — 1 10.57
CHEMBL4776758 — — 1 10.55
CHEMBL4746184 — — 1 10.51
CHEMBL4740465 — — 1 10.51
CHEMBL4797225 — — 1 10.49
CHEMBL4471306 QUEMLICLUSTAT 2.0 1 10.39
CHEMBL4743437 — — 1 10.35
CHEMBL4790144 — — 1 10.28
CHEMBL4745002 — — 1 10.24
CHEMBL4784155 — — 1 10.15
CHEMBL4777161 — — 1 10.02
CHEMBL4761506 — — 1 9.94
CHEMBL4753354 — — 1 9.92
CHEMBL4763896 — — 1 9.82
CHEMBL4758486 — — 1 9.82
CHEMBL4744502 — — 1 9.70
CHEMBL4780231 — — 1 9.52
CHEMBL4788910 — — 1 9.52
CHEMBL4748647 — — 1 9.40
CHEMBL4748576 — — 1 9.22
CHEMBL4779616 — — 1 9.15
CHEMBL4750588 — — 1 9.15
CHEMBL4746820 — — 1 9.15
CHEMBL4761534 — — 1 9.10
CHEMBL4741516 — — 1 9.05
CHEMBL4755101 — — 1 8.96
CHEMBL4759136 — — 1 8.89
CHEMBL4793370 — — 1 8.89
CHEMBL4796737 — — 1 8.89
CHEMBL4753731 — — 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4749428 — IC50 = 0.027 nM 10.57
CHEMBL4776758 — IC50 = 0.028 nM 10.55
CHEMBL4740465 — IC50 = 0.031 nM 10.51
CHEMBL4746184 — IC50 = 0.031 nM 10.51
CHEMBL4797225 — IC50 = 0.032 nM 10.49
CHEMBL4471306 QUEMLICLUSTAT IC50 = 0.041 nM 10.39
CHEMBL4743437 — IC50 = 0.045 nM 10.35
CHEMBL4790144 — IC50 = 0.052 nM 10.28
CHEMBL4745002 — IC50 = 0.058 nM 10.24
CHEMBL4784155 — IC50 = 0.07 nM 10.15
CHEMBL4777161 — IC50 = 0.095 nM 10.02
CHEMBL4761506 — IC50 = 0.115 nM 9.94
CHEMBL4753354 — IC50 = 0.12 nM 9.92
CHEMBL4758486 — IC50 = 0.15 nM 9.82
CHEMBL4763896 — IC50 = 0.15 nM 9.82
CHEMBL4744502 — IC50 = 0.2 nM 9.70
CHEMBL4780231 — IC50 = 0.3 nM 9.52
CHEMBL4788910 — IC50 = 0.3 nM 9.52
CHEMBL4748647 — IC50 = 0.4 nM 9.40
CHEMBL4748576 — IC50 = 0.6 nM 9.22
CHEMBL4779616 — IC50 = 0.7 nM 9.15
CHEMBL4750588 — IC50 = 0.7 nM 9.15
CHEMBL4746820 — IC50 = 0.7 nM 9.15
CHEMBL4761534 — IC50 = 0.8 nM 9.10
CHEMBL4741516 — IC50 = 0.9 nM 9.05
CHEMBL4755101 — IC50 = 1.1 nM 8.96
CHEMBL4793370 — IC50 = 1.3 nM 8.89
CHEMBL4796737 — IC50 = 1.3 nM 8.89
CHEMBL4759136 — IC50 = 1.3 nM 8.89
CHEMBL4753731 — IC50 = 1.4 nM 8.85
CHEMBL4763785 — IC50 = 1.5 nM 8.82
CHEMBL4748342 — IC50 = 1.6 nM 8.80
CHEMBL4776829 — IC50 = 1.7 nM 8.77
CHEMBL4760025 — IC50 = 2.0 nM 8.70
CHEMBL4784883 — IC50 = 2.1 nM 8.68
CHEMBL4791467 — IC50 = 2.2 nM 8.66
CHEMBL4796788 — IC50 = 2.4 nM 8.62
CHEMBL4783528 — IC50 = 2.6 nM 8.59
CHEMBL4744406 — IC50 = 3.3 nM 8.48
CHEMBL4287314 — IC50 = 3.4 nM 8.47
CHEMBL4747191 — IC50 = 3.6 nM 8.44
CHEMBL4751771 — IC50 = 3.6 nM 8.44
CHEMBL4748492 — IC50 = 4.0 nM 8.40
CHEMBL4779193 — IC50 = 4.1 nM 8.39
CHEMBL4784405 — IC50 = 4.2 nM 8.38
CHEMBL4755896 — IC50 = 5.0 nM 8.30
CHEMBL4475460 — IC50 = 5.0 nM 8.30
CHEMBL4752232 — IC50 = 5.0 nM 8.30
CHEMBL4742951 — IC50 = 5.4 nM 8.27
CHEMBL4752494 — IC50 = 5.9 nM 8.23