Table 11Physical Properties of the Heteroaromatic Surrogates

Image ml189fu10.jpg
Purity (%)PBS Solubility at 23 °C (μM)Plasma Protein Binding (% bound)Plasma Stability (% remaining after 5 hrs)
No.CIDSIDBroad Internal Number*Heterocycle
1410148499376502BRD-K02364554SH>99384Human12Human77
Mouse5.7Mouse81
22584891199376538BRD-K23419995S1-methyl-1H- imidazol-2-yl92480Human49HumanND
Mouse56MouseND
31752379199376557BRD-K58038195S2-thiazolyl66104Human87Human98
Mouse78Mouse91
489716799245561BRD-K41809803Pp-Cl-C6H498<1.0Human>99Human87
Mouse98Mouse84
587037199245569BRD-K68535470P2-pyridyl>99415Human87Human95
Mouse82Mouse98
99376529S>99309Human87Human>99
Mouse83Mouse97
64691214799376521BRD-K77258719S3-pyridyl97426Human68Human>99
Mouse69Mouse99
7904829699376503BRD-K44472748S4-pyridyl99392Human39Human83
Mouse41Mouse94
84691218599376554BRD-K09269542S6-trifluoromethyl- pyrid-2-yl994.3Human99HumanND
Mouse98MouseND
94691218499376537BRD-K97452196S6-methyl-pyrid-2-yl95NDHumanNDHumanND
MouseNDMouseND
1072706099376553BRD-K70285947S2-pyrimidinyl>99178Human82HumanND
Mouse76MouseND
114181215799376545BRD-K11064892S2-pyrazinyl>99481Human71HumanND
Mouse59MouseND
124691217299376552BRD-K74514012S6-methyl-pyridazin-3-yl>99391Human70HumanND
Mouse76MouseND
13125213399245570BRD-K23406875P5,8-dimethoxy-4-methylquinolin-2-yl97<1.0Human>99Human95
Mouse>99Mouse89
144691215399376515BRD-K97337830S4-quinazolinyl99221Human92Human>99
Mouse87Mouse97
153791989599376533BRD-K40981928Sbenzo[d]oxazol-2-yl>991.1Human96HumanND
Mouse93MouseND
*

S = synthesized P = purchased ND = not determined

S = synthesized P = purchased ND = not determined

From: Identification of small molecules that selectively inhibit fluconazole-resistant Candida albicans in the presence of fluconazole but not in its absence

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

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