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Assay Detail

CHEMBL2382691

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

Binding
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
31
Total Activities
31
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

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.
Stössel A, Schlenk M, Hinz S, Küppers P, Heer J, Gütschow M, Müller CE.
J Med Chem (2013) 56 : 4580 -4596
PubMed 23631427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 6.43 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2382438 1 6.92
CHEMBL2380386 1 6.65
CHEMBL2382435 1 6.52
CHEMBL2382425 1 6.44
CHEMBL2380385 1 6.44
CHEMBL2382420 1 6.39
CHEMBL2382424 1 6.26
CHEMBL2382431 1 6.17
CHEMBL2382428 1 6.10
CHEMBL2382437 1 -
CHEMBL2382439 1 -
CHEMBL2382440 1 -
CHEMBL2382441 1 -
CHEMBL2380381 1 -
CHEMBL2380382 1 -
CHEMBL2380383 1 -
CHEMBL2380384 1 -
CHEMBL2382421 1 -
CHEMBL2382422 1 -
CHEMBL2382436 1 -
CHEMBL2382434 1 -
CHEMBL431770 ISTRADEFYLLINE 4.0 1 -
CHEMBL2382433 1 -
CHEMBL2382432 1 -
CHEMBL2382430 1 -
CHEMBL2382429 1 -
CHEMBL2382427 1 -
CHEMBL2382426 1 -
CHEMBL26138 1 -
CHEMBL240624 PRELADENANT 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2382438 Ki = 119.0 nM 6.92
CHEMBL2380386 Ki = 225.0 nM 6.65
CHEMBL2382435 Ki = 302.0 nM 6.52
CHEMBL2382425 Ki = 361.0 nM 6.44
CHEMBL2380385 Ki = 365.0 nM 6.44
CHEMBL2382420 Ki = 408.0 nM 6.39
CHEMBL2382424 Ki = 547.0 nM 6.26
CHEMBL2382431 Ki = 679.0 nM 6.17
CHEMBL2382428 Ki = 801.0 nM 6.10
CHEMBL2382437 Ki > 1000.0 nM -
CHEMBL2382423 Ki > 1000.0 nM -
CHEMBL2382439 Ki >= 1000.0 nM -
CHEMBL2382440 Ki > 1000.0 nM -
CHEMBL2382441 Ki > 1000.0 nM -
CHEMBL2380381 Ki > 1000.0 nM -
CHEMBL2380382 Ki > 1000.0 nM -
CHEMBL2380383 Ki > 1000.0 nM -
CHEMBL2380384 Ki > 1000.0 nM -
CHEMBL2382421 Ki > 1000.0 nM -
CHEMBL2382422 Ki > 1000.0 nM -
CHEMBL2382436 Ki >= 1000.0 nM -
CHEMBL2382434 Ki > 1000.0 nM -
CHEMBL431770 ISTRADEFYLLINE Ki > 10000.0 nM -
CHEMBL2382433 Ki > 1000.0 nM -
CHEMBL2382432 Ki > 1000.0 nM -
CHEMBL2382430 Ki > 1000.0 nM -
CHEMBL2382429 Ki > 1000.0 nM -
CHEMBL2382427 Ki > 1000.0 nM -
CHEMBL2382426 Ki > 1000.0 nM -
CHEMBL26138 Ki > 1000.0 nM -
CHEMBL240624 PRELADENANT Ki > 1000.0 nM -