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Assay Detail

CHEMBL3129538

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

Binding
Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydrase assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 12 (CHEMBL3242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and evaluation of N-substituted saccharin derivatives as selective inhibitors of tumor-associated carbonic anhydrase XII.
D'Ascenzio M, Carradori S, De Monte C, Secci D, Ceruso M, Supuran CT.
Bioorg Med Chem (2014) 22 : 1821 -1831
PubMed 24560739 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 6.50 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 8.22
CHEMBL3125544 1 7.68
CHEMBL3125542 1 7.61
CHEMBL3125543 1 7.60
CHEMBL1545298 1 7.55
CHEMBL1470455 1 7.55
CHEMBL3125555 1 7.38
CHEMBL3125563 1 7.12
CHEMBL3125561 1 7.03
CHEMBL3125564 1 6.82
CHEMBL3125562 1 6.68
CHEMBL3125554 1 6.62
CHEMBL3125553 1 6.62
CHEMBL3125556 1 6.60
CHEMBL415079 1 6.36
CHEMBL3125560 1 6.24
CHEMBL310671 SACCHARIN 3.0 1 6.20
CHEMBL3125559 1 6.15
CHEMBL3125551 1 6.01
CHEMBL3125547 1 5.88
CHEMBL1450780 1 5.75
CHEMBL3125552 1 5.70
CHEMBL3125545 1 5.60
CHEMBL3125549 1 5.59
CHEMBL3125546 1 5.57
CHEMBL3125548 1 5.56
CHEMBL1603618 1 5.54
CHEMBL3125550 1 4.87
CHEMBL131790 1 -
CHEMBL3125557 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 6.0 nM 8.22
CHEMBL3125544 Ki = 21.1 nM 7.68
CHEMBL3125542 Ki = 24.6 nM 7.61
CHEMBL3125543 Ki = 25.1 nM 7.60
CHEMBL1545298 Ki = 28.4 nM 7.55
CHEMBL1470455 Ki = 28.1 nM 7.55
CHEMBL3125555 Ki = 41.9 nM 7.38
CHEMBL3125563 Ki = 76.5 nM 7.12
CHEMBL3125561 Ki = 94.0 nM 7.03
CHEMBL3125564 Ki = 150.0 nM 6.82
CHEMBL3125562 Ki = 210.0 nM 6.68
CHEMBL3125554 Ki = 240.0 nM 6.62
CHEMBL3125553 Ki = 240.0 nM 6.62
CHEMBL3125556 Ki = 250.0 nM 6.60
CHEMBL415079 Ki = 440.0 nM 6.36
CHEMBL3125560 Ki = 570.0 nM 6.24
CHEMBL310671 SACCHARIN Ki = 633.0 nM 6.20
CHEMBL3125559 Ki = 710.0 nM 6.15
CHEMBL3125551 Ki = 970.0 nM 6.01
CHEMBL3125547 Ki = 1310.0 nM 5.88
CHEMBL1450780 Ki = 1780.0 nM 5.75
CHEMBL3125552 Ki = 2010.0 nM 5.70
CHEMBL3125545 Ki = 2520.0 nM 5.60
CHEMBL3125549 Ki = 2540.0 nM 5.59
CHEMBL3125546 Ki = 2690.0 nM 5.57
CHEMBL3125548 Ki = 2760.0 nM 5.56
CHEMBL1603618 Ki = 2910.0 nM 5.54
CHEMBL3125550 Ki = 13410.0 nM 4.87
CHEMBL131790 Ki > 50000.0 nM -
CHEMBL3125557 Ki > 50000.0 nM -
CHEMBL3125558 Ki > 50000.0 nM -